We provide robust and sensitive in vitro screening and characterization platforms for accelerating the discovery and screening of potential therapies for Bladder Cancer. Our service offers comprehensive efficacy profiling of candidate compounds using bladder cancer-relevant cellular and molecular models. Key targets include growth factor receptors, immune checkpoints such as PD-1, and androgen receptor pathways, all of which play crucial roles in bladder cancer progression and therapeutic response. We are equipped to assess processes such as tumor cell proliferation, receptor binding, immune modulation, and signal transduction relevant to bladder cancer pathology.
Our in vitro testing portfolio encompasses a wide array of biochemical, cell-based, and binding assays designed to evaluate drug efficacy, mechanism of action, and target engagement in bladder cancer models. These methods enable precise quantification of cellular responses, receptor interactions, and pathway modulation, supporting comprehensive preclinical candidate evaluation.
ATP assay: Measures cellular viability and proliferation by quantifying ATP levels, indicating cytotoxic or cytostatic effects of candidate compounds.
ATP assay (at 0.01 mM): Evaluates compound efficacy at low concentration, providing sensitivity for early potency assessment.
ATP assay (at 1 mM): Assesses compound activity at higher concentrations to determine dose-response relationships.
Biolayer interferometry assay: Analyzes real-time biomolecular interactions, such as ligand-receptor binding kinetics relevant to bladder cancer targets.
Cell counting assay (with charcoal-stripped serum-treated): Quantifies cell proliferation under hormone-depleted conditions, useful for studying androgen or hormone-responsive pathways.
Cells (effector) transfected with PD1: Models immune checkpoint interactions, allowing assessment of immunotherapeutic modulators targeting PD-1.
Chemiluminescent assay: Detects biological activity through luminescence, often used for enzyme or reporter gene assays.
Competitive binding assay: Determines the ability of compounds to displace labeled ligands, providing insights into binding affinity and specificity.
Displacement of [3H]-mibolerone: Measures androgen receptor binding by quantifying displacement of a radiolabeled ligand, relevant for hormone pathway studies.
Dissociation enhanced lanthanide fluorescent immunoassay (DELFIA): Enables highly sensitive detection of biomolecules using time-resolved fluorescence, suitable for receptor-ligand or protein quantification.
ELISA assay: Quantifies proteins, cytokines, or biomarkers in cell supernatants, critical for monitoring cellular responses and signaling events.
Flow cytometry assay: Analyzes cell populations and surface or intracellular markers, facilitating detailed phenotypic and functional characterization.
Fluorescence resonance energy transfer (FRET) assay: Detects molecular interactions or conformational changes within live cells or in vitro systems.
Fluorescent assay: Measures cellular or enzymatic activity using fluorescent substrates or probes.
Fluorescent polarization assay: Assesses molecular binding events by detecting changes in fluorescence polarization, useful for small molecule or peptide interactions.
Fluorescent-activated cell sorting (FACS) assay: Allows high-throughput sorting and analysis of distinct cell populations based on fluorescence markers.
Homogeneous Time Resolved Fluorescence (HTRF) assay: Combines FRET and time-resolved fluorescence for sensitive and quantitative detection of biomolecular interactions.
Jurkat human T-cell leukemia cells transfected with PD1/NFAT/luciferase: Provides a functional immune cell model to evaluate effects on PD-1 and downstream signaling.
Jurkat human T-cell leukemia cells transfected with human PD1/NFAT/luciferase: Similar to above, specifically utilizing human PD-1 for assessing human-specific immune responses.
Luciferine/luciferase assay: Measures gene expression or reporter activity via bioluminescence, indicating cellular pathway activation or inhibition.
Poly(L-alanine/L-glutamic acid/L-lysine/L-tyrosine) as substrate: Used in enzymatic assays to evaluate protease or kinase activity relevant to cancer signaling.
Poly(glutamine/tyrosine) peptide as substrate: Serves as a substrate for characterizing enzyme specificity and activity in signaling pathways.
RNA assay: Quantifies gene expression changes in response to treatment, providing insight into mechanism of action and target modulation.
Radioactivity assay: Utilizes radiolabeled compounds for sensitive detection of molecular or cellular events.
Surface plasmon resonance assay: Measures real-time binding kinetics and affinity between molecules, supporting characterization of drug-target interactions.
Transactivation assay: Evaluates the ability of compounds to modulate transcriptional activity of nuclear receptors or transcription factors.
We measure a comprehensive set of pharmacological parameters, including potency, efficacy, binding affinity, and inhibitory concentration, to thoroughly characterize candidate compounds. These parameters are vital for understanding drug activity, optimizing therapeutic windows, and supporting decision-making in lead selection. Accurate parameter measurement ensures reliable prediction of in vivo efficacy and safety.
EC-50: The concentration of a compound that produces 50% of its maximal effect, indicating drug potency.
IC-50: The concentration required to inhibit a specific biological or biochemical function by 50%, widely used to assess inhibitory activity.
Kd: The equilibrium dissociation constant reflecting the affinity between a drug and its target, with lower values indicating stronger binding.
Ki: The inhibition constant representing the potency of an inhibitor binding to an enzyme or receptor, crucial for characterizing competitive inhibitors.
MEC: Minimum effective concentration, the lowest concentration at which a compound exerts a measurable effect, important for dosing considerations.
MIC: Minimum inhibitory concentration, the lowest concentration that prevents detectable growth of target cells or organisms, key for anti-proliferative agents.
pIC-50: The negative logarithm of the IC-50 value, providing a standardized and easily comparable measure of inhibitor potency.
Androgen Receptor (AR) plays a regulatory role in bladder cancer progression, influencing tumor growth and therapy response. AR testing is crucial for identifying drug candidates that modulate AR activity. Our service employs advanced methods—including chemiluminescent, fluorescent, and luciferase assays, transactivation, competitive binding, [3H]-mibolerone displacement, cell counting, and RNA assays—to measure key parameters: EC-50, Ki, MIC, and IC-50, ensuring precise assessment of AR-targeted drug efficacy.
Pharmacological Activity | Material | Method | Parameter |
---|---|---|---|
Androgen AR receptor (W741C-mutated) activation (dihydrotestosterone-induced), inhibition | LNCaP human prostate carcinoma cells (androgen-dependent) transfected with ARR(2)PB/eGFP | Fluorescent assay | IC-50 |
Androgen AR receptor (variant V7) degradation, induction | 22Rv1 human prostate carcinoma cells | Chemiluminescent assay | EC-50 |
Androgen AR receptor activation (dihydrotestosterone-induced), inhibition | HEK293T human embryonic kidney cells | Luciferine/luciferase assay | IC-50 |
Androgen AR receptor activation (dihydrotestosterone-induced), inhibition | LNCaP human prostate carcinoma cells (androgen-dependent) transfected with ARR(2)PB/eGFP | Fluorescent assay | IC-50 |
Androgen AR receptor activation (dihydrotestosterone-induced), inhibition | LNCaP human prostate carcinoma cells (androgen-dependent) transfected with eGFP | Fluorescent assay | IC-50 |
Androgen AR receptor activation, inhibition | HEK293 human embryonic kidney cells transfected with human receptor/luciferase | Luciferine/luciferase assay | IC-50 |
Androgen AR receptor activation, inhibition | HEK293 human embryonic kidney cells transfected with human receptor/luciferase | Transactivation assay | IC-50 |
Androgen AR receptor affinity | LNCaP human prostate carcinoma cells (androgen-dependent) | Radioactivity assay | IC-50 |
Androgen AR receptor affinity | LNCaP human prostate carcinoma cells (androgen-dependent) | IC-50 | |
Androgen AR receptor affinity | Prostate, rat (castrated) | Displacement of [3H]-mibolerone | Ki |
Androgen AR receptor affinity | Recombinant human receptor | Competitive binding assay | IC-50 |
Androgen AR receptor affinity | Fluorescent polarization assay | IC-50 | |
Androgen AR receptor downregulation, induction | LNCaP human prostate carcinoma cells (androgen-dependent) | EC-50 | |
Gene (androgen AR receptor variant V7) transcription (dihydrotestosterone-induced), inhibition | HEK293T human embryonic kidney cells | Luciferine/luciferase assay | IC-50 |
Gene (androgen AR receptor) (E255K-mutated) transcription (dihydrotestosterone-induced), inhibition | HEK293T human embryonic kidney cells | Luciferine/luciferase assay | IC-50 |
Gene (androgen AR receptor) (F887L/T878A-mutated) transcription (dihydrotestosterone-induced), inhibition | HEK293T human embryonic kidney cells | Luciferine/luciferase assay | IC-50 |
Gene (androgen AR receptor) (H875Y/T878S-mutated) transcription (dihydrotestosterone-induced), inhibition | HEK293T human embryonic kidney cells | Luciferine/luciferase assay | IC-50 |
Gene (androgen AR receptor) (L702H-mutated) transcription (dihydrotestosterone-induced), inhibition | HEK293T human embryonic kidney cells | Luciferine/luciferase assay | IC-50 |
Gene (androgen AR receptor) (W435L-mutated) transcription (dihydrotestosterone-induced), inhibition | HEK293T human embryonic kidney cells | Luciferine/luciferase assay | IC-50 |
Gene (androgen AR receptor) (W742C-mutated) transcription (dihydrotestosterone-induced), inhibition | HEK293T human embryonic kidney cells | Luciferine/luciferase assay | IC-50 |
Gene (androgen AR receptor) (W742C-mutated) transcription (dihydrotestosterone-induced), inhibition | LNCaP human prostate carcinoma cells (androgen-dependent) transfected with eGFP | RNA assay | IC-50 |
Gene (androgen AR receptor) transcription (cortisol-induced), inhibition | HEK293 human embryonic kidney cells (androgen receptor (L702H)-mutated) | Luciferine/luciferase assay | IC-50 |
Gene (androgen AR receptor) transcription (dihydrotestosterone-induced), inhibition | HEK293T human embryonic kidney cells | Luciferine/luciferase assay | IC-50 |
Gene (androgen AR receptor) transcription (dihydrotestosterone-induced), inhibition | LNCaP human prostate carcinoma cells (androgen-dependent) | RNA assay | MIC |
Gene (androgen AR receptor) transcription (dihydrotestosterone-induced), inhibition | LNCaP human prostate carcinoma cells (androgen-dependent) transfected with ARR(2)PB/eGFP | Fluorescent assay | IC-50 |
Gene (androgen AR receptor) transcription (metribolone-induced), inhibition | HEK293 human embryonic kidney cells | Luciferine/luciferase assay | IC-50 |
Gene (androgen AR receptor) transcription (metribolone-induced), inhibition | HEK293 human embryonic kidney cells (androgen receptor (L702H)-mutated) | Luciferine/luciferase assay | IC-50 |
Gene (androgen AR receptor) transcription (prednisolone-induced), inhibition | HEK293 human embryonic kidney cells (androgen receptor (L702H)-mutated) | Luciferine/luciferase assay | IC-50 |
Gene (androgen AR receptor) transcription, inhibition | LNCaP human prostate carcinoma cells (androgen-dependent) | RNA assay | IC-50 |
Gene (androgen AR receptor) transcription, inhibition | LNCaP human prostate carcinoma cells (androgen-dependent) transfected with PSA/renilla luciferase | Luciferine/luciferase assay | IC-50 |
Gene transcription (AR receptor-dependent) (metribolone-induced), inhibition | LNCaP human prostate carcinoma cells (androgen-dependent) transfected with PSA/luciferase | Luciferine/luciferase assay | IC-50 |
Mitogenesis (cortisol-induced), inhibition | MDAPCa2b human prostate adenocarcinoma cells (androgen receptor (T878A/L702H)-mutated) | Cell counting assay (with charcoal-stripped serum-treated) | IC-50 |
Mitogenesis (cortisone-induced), inhibition | MDAPCa2b human prostate adenocarcinoma cells (androgen receptor (T878A/L702H)-mutated) | Cell counting assay (with charcoal-stripped serum-treated) | IC-50 |
Mitogenesis (metribolone-induced), inhibition | MDAPCa2b human prostate adenocarcinoma cells (androgen receptor (T878A/L702H)-mutated) | Cell counting assay (with charcoal-stripped serum-treated) | IC-50 |
Prostate-specific antigen (PSA) production (dihydrotestosterone-induced), inhibition | LNCaP human prostate carcinoma cells (androgen-dependent) transfected with ARR(2)PB/eGFP | IC-50 |
The Cd274 molecule (PD-L1) is crucial in bladder cancer progression by helping tumor cells evade immune detection. Testing Cd274 is vital for drug development targeting immune checkpoints. Our service utilizes advanced methods—including FACS, flow cytometry, chemiluminescent, fluorescent, SPR, biolayer interferometry, ELISA, and engineered Jurkat T-cell assays—to evaluate drug efficacy. Key parameters measured include IC-50, Kd, MIC, EC-50, and MEC, ensuring robust preclinical immunotherapy assessment.
Pharmacological Activity | Material | Method | Parameter |
---|---|---|---|
B7-H1 (CD274 antigen, PDL1) affinity | CHO Chinese hamster ovary cells (CD274-overexpressing) | Flow cytometry assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | CHO Chinese hamster ovary cells (CD274-overexpressing) | Fluorescent-activated cell sorting (FACS) assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | CHO Chinese hamster ovary cells transfected with human protein | Fluorescent assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | CHO Chinese hamster ovary cells transfected with protein | Flow cytometry assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | CHO-S Chinese hamster ovary cells transfected with human protein | Flow cytometry assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | Cynomolgus monkey protein | Biolayer interferometry assay | Kd |
B7-H1 (CD274 antigen, PDL1) affinity | Cynomolgus monkey protein | ELISA assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | HEK293T human embryonic kidney cells transfected with mouse protein | Flow cytometry assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | Hepa1-6 mouse hepatoma cells | Flow cytometry assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | Human protein | Biolayer interferometry assay | Kd |
B7-H1 (CD274 antigen, PDL1) affinity | Human protein | ELISA assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | Human protein | Flow cytometry assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | Human protein | Surface plasmon resonance assay | Kd |
B7-H1 (CD274 antigen, PDL1) affinity | Human protein | IC-50 | |
B7-H1 (CD274 antigen, PDL1) affinity | Mouse protein | IC-50 | |
B7-H1 (CD274 antigen, PDL1) affinity | NCI-H441 human lung papillary adenocarcinoma cells | Flow cytometry assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | Recombinant cynomolgus monkey protein | Biolayer interferometry assay | Kd |
B7-H1 (CD274 antigen, PDL1) affinity | Recombinant human protein | Biolayer interferometry assay | Kd |
B7-H1 (CD274 antigen, PDL1) affinity | Recombinant human protein | ELISA assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | Recombinant human protein | Surface plasmon resonance assay | Kd |
B7-H1 (CD274 antigen, PDL1) affinity | Recombinant mouse protein | Biolayer interferometry assay | Kd |
B7-H1 (CD274 antigen, PDL1) affinity | Recombinant protein | ELISA assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | Recombinant rhesus monkey protein | Biolayer interferometry assay | Kd |
B7-H1 (CD274 antigen, PDL1) affinity | T24 human bladder transitional-cell carcinoma cells | Flow cytometry assay | IC-50 |
B7-H1 (CD274 antigen, PDL1) affinity | Biolayer interferometry assay | Kd | |
B7-H1 (CD274 antigen, PDL1) affinity | Kd | ||
B7-H1 (CD274 antigen, PDL1) expression, induction | FaDu human squamous-cell nasopharyngeal cancer cells | Chemiluminescent assay | MEC |
B7-H1 (CD274 antigen, PDL1) expression, induction | EC-50 | ||
B7-H1 (CD274 antigen, PDL1) expression, inhibition | B16F10 mouse metastatic melanoma cells | Chemiluminescent assay | MIC |
B7-H1 (CD274 antigen, PDL1)/Programmed cell death 1 (PD-1) interaction, inhibition | CHO Chinese hamster ovary cells (CD274-overexpressing) | Jurkat human T-cell leukemia cells transfected with PD1/NFAT/luciferase | IC-50 |
B7-H1 (CD274 antigen, PDL1)/Programmed cell death 1 (PD-1) interaction, inhibition | CHO Chinese hamster ovary cells transfected with human CD274 | Jurkat human T-cell leukemia cells transfected with human PD1/NFAT/luciferase | IC-50 |
B7-H1 (CD274 antigen, PDL1)/Programmed cell death 1 (PD-1) interaction, inhibition | CHO-K1 Chinese hamster ovary cells transfected with human CD274 | Jurkat human T-cell leukemia cells transfected with PD1/NFAT/luciferase | IC-50 |
B7-H1 (CD274 antigen, PDL1)/Programmed cell death 1 (PD-1) interaction, inhibition | CHO-K1 Chinese hamster ovary cells transfected with human protein | Fluorescent-activated cell sorting (FACS) assay | IC-50 |
Programmed cell death 1 (PD-1)/B7-H1 (CD274 antigen, PDL1) complex interaction, inhibition | CHO Chinese hamster ovary cells transfected with human protein | Flow cytometry assay | IC-50 |
Programmed cell death 1 (PD-1)/B7-H1 (CD274 antigen, PDL1) complex interaction, inhibition | CHO-K1 Chinese hamster ovary cells transfected with CD274/aAPC | Cells (effector) transfected with PD1 | IC-50 |
Programmed cell death 1 (PD-1)/B7-H1 (CD274 antigen, PDL1) complex interaction, inhibition | CHO-K1 Chinese hamster ovary cells transfected with CD274/aAPC | Jurkat human T-cell leukemia cells transfected with PD1/NFAT/luciferase | IC-50 |
Dihydrofolate Reductase (DHFR) is a key enzyme in DNA synthesis, often upregulated in bladder cancer, making it a vital drug target. DHFR testing is crucial for evaluating drug efficacy and resistance. Our service employs enzymatic assays, gene expression analysis, and inhibitor screening. Main parameters assessed include DHFR activity, mRNA/protein levels, and IC50 values for candidate compounds—essential for informed drug development in bladder cancer.
Pharmacological Activity | Parameter |
---|---|
Dihydrofolate reductase, inhibition | IC-50 |
DNA Topoisomerase I is crucial for DNA replication and is often overexpressed in bladder cancer, making it a key drug target. Testing its activity helps evaluate drug efficacy and resistance. Our service uses a sensitive chemiluminescent assay to quantify Topoisomerase I inhibition. The main parameter measured is the Minimum Inhibitory Concentration (MIC), enabling precise assessment of candidate drug potency during bladder cancer drug development.
Pharmacological Activity | Material | Method | Parameter |
---|---|---|---|
DNA topoisomerase I expression, inhibition | LoVo human colon adenocarcinoma cells | Chemiluminescent assay | MIC |
DNA topoisomerase I expression, inhibition | LoVo human colon adenocarcinoma cells (irinotecan-resistant) | Chemiluminescent assay | MIC |
Epidermal Growth Factor Receptor (EGFR) plays a pivotal role in bladder cancer progression by driving cell proliferation and survival. EGFR testing is essential in drug development to identify and evaluate targeted therapies. Our service utilizes advanced methods—FACS, DELFIA, chemiluminescent, HTRF, FRET, SPR, ELISA, and ATP/fluorescent assays—to assess drug efficacy and interaction. Key parameters measured include IC-50, MIC, Kd, pIC-50, and MEC for comprehensive candidate profiling.
Pharmacological Activity | Material | Method | Parameter |
---|---|---|---|
Epidermal growth factor EGF receptor (EGFR) degradation, induction | CCK81 human colon adenocarcinoma cells | Fluorescent assay | MEC |
Epidermal growth factor EGF receptor (EGFR) degradation, induction | HCT8 human ileocecal adenocarcinoma cells | Fluorescent assay | MEC |
Protein-tyrosine kinase (EGF receptor) (A263P-mutated], inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor) (A289D-mutated], inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor) (A289V-mutated], inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor) (G598V-mutated], inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor) (L858R-mutated), inhibition | Recombinant enzyme | Fluorescence resonance energy transfer (FRET) assay | IC-50 |
Protein-tyrosine kinase (EGF receptor) (L858R-mutated), inhibition | Recombinant human enzyme | ATP assay | IC-50 |
Protein-tyrosine kinase (EGF receptor) (L858R-mutated), inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor) (L858R/C797S-mutated), inhibition | Recombinant enzyme | Fluorescence resonance energy transfer (FRET) assay | IC-50 |
Protein-tyrosine kinase (EGF receptor) (L858R/C797S-mutated), inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor) (L858R/T790M-mutated), inhibition | Recombinant enzyme | Fluorescence resonance energy transfer (FRET) assay | IC-50 |
Protein-tyrosine kinase (EGF receptor) (L858R/T790M-mutated), inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor) (L858R/T790M/C797S-mutated), inhibition | Recombinant enzyme | Fluorescence resonance energy transfer (FRET) assay | IC-50 |
Protein-tyrosine kinase (EGF receptor) (L858R/T790M/C797S-mutated), inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor) (T790M-mutated), inhibition | Recombinant human enzyme | ATP assay | IC-50 |
Protein-tyrosine kinase (EGF receptor) (T790M-mutated), inhibition | Homogeneous Time Resolved Fluorescence (HTRF) assay | IC-50 | |
Protein-tyrosine kinase (EGF receptor) (exon 19-deleted), inhibition | Recombinant human enzyme | ATP assay | IC-50 |
Protein-tyrosine kinase (EGF receptor) (exon 19-deleted), inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor) (exon 19-deleted/C797S-mutated), inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor) (exon 19-deleted/T790M-mutated), inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor) (exon 19-deleted/T790M/C797S-mutated), inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor) (variant III-mutated), inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor) affinity | CT26 murine colon adenocarcinoma cells | Fluorescent-activated cell sorting (FACS) assay | IC-50 |
Protein-tyrosine kinase (EGF receptor) affinity | Recombinant cynomolgus monkey enzyme | Surface plasmon resonance assay | Kd |
Protein-tyrosine kinase (EGF receptor) affinity | Recombinant human enzyme | Surface plasmon resonance assay | Kd |
Protein-tyrosine kinase (EGF receptor) affinity | Surface plasmon resonance assay | Kd | |
Protein-tyrosine kinase (EGF receptor) phosphorylation, induction | MDAMB453 human breast carcinoma cells | Chemiluminescent assay | MEC |
Protein-tyrosine kinase (EGF receptor) phosphorylation, inhibition | FaDu human squamous-cell nasopharyngeal cancer cells | Chemiluminescent assay | MIC |
Protein-tyrosine kinase (EGF receptor) phosphorylation, inhibition | MDAMB453 human breast carcinoma cells (HER2 [ERBB2]-overexpressing) | Chemiluminescent assay | MIC |
Protein-tyrosine kinase (EGF receptor) phosphorylation, inhibition | NCI-H2073 human non-small-cell lung adenocarcinoma cells | Homogeneous Time Resolved Fluorescence (HTRF) assay | pIC-50 |
Protein-tyrosine kinase (EGF receptor) phosphorylation, inhibition | SKBr3 human breast adenocarcinoma cells (HER2 [ERBB2]-overexpressing) | Chemiluminescent assay | MIC |
Protein-tyrosine kinase (EGF receptor) phosphorylation, inhibition | IC-50 | ||
Protein-tyrosine kinase (EGF receptor), inhibition | BAF3 mouse lymphoblasts (epidermal growth factor-treated) | IC-50 | |
Protein-tyrosine kinase (EGF receptor), inhibition | Human enzyme | ATP assay | IC-50 |
Protein-tyrosine kinase (EGF receptor), inhibition | PC3 human prostate adenocarcinoma cells | ATP assay | IC-50 |
Protein-tyrosine kinase (EGF receptor), inhibition | Recombinant enzyme | ATP assay (at 0.01 mM) | pIC-50 |
Protein-tyrosine kinase (EGF receptor), inhibition | Recombinant enzyme | ATP assay (at 1 mM) | pIC-50 |
Protein-tyrosine kinase (EGF receptor), inhibition | Recombinant enzyme | Chemiluminescent assay | IC-50 |
Protein-tyrosine kinase (EGF receptor), inhibition | Recombinant enzyme | Dissociation enhanced lanthanide fluorescent immunoassay (DELFIA) | IC-50 |
Protein-tyrosine kinase (EGF receptor), inhibition | Recombinant enzyme | Fluorescence resonance energy transfer (FRET) assay | IC-50 |
Protein-tyrosine kinase (EGF receptor), inhibition | Recombinant enzyme | Poly(glutamine/tyrosine) peptide as substrate | pIC-50 |
Protein-tyrosine kinase (EGF receptor), inhibition | Recombinant human enzyme | ATP assay | IC-50 |
Protein-tyrosine kinase (EGF receptor), inhibition | Recombinant human enzyme | ELISA assay | IC-50 |
Protein-tyrosine kinase (EGF receptor), inhibition | Sf9 insect cells transfected with enzyme | ATP assay | IC-50 |
Protein-tyrosine kinase (EGF receptor), inhibition | Chemiluminescent assay | IC-50 | |
Protein-tyrosine kinase (EGF receptor), inhibition | ELISA assay | IC-50 | |
Protein-tyrosine kinase (EGF receptor), inhibition | Fluorescence resonance energy transfer (FRET) assay | IC-50 | |
Protein-tyrosine kinase (EGF receptor), inhibition | IC-50 |
Erb-B2 Receptor Tyrosine Kinase 2 (HER2/ERBB2) plays a pivotal role in bladder cancer progression and therapy resistance. Testing its expression and activity is crucial for targeted drug development. Our service utilizes advanced methods—FACS, chemiluminescent, flow cytometry, FRET, surface plasmon resonance, biolayer interferometry, and ELISA assays—to assess key parameters, including MEC, Kd, IC-50, and MIC, enabling precise evaluation of candidate therapeutics.
Pharmacological Activity | Material | Method | Parameter |
---|---|---|---|
Protein-tyrosine kinase (HER2 [ErbB2]) (extracellular domain 4) affinity | Surface plasmon resonance assay | Kd | |
Protein-tyrosine kinase (HER2 [ErbB2]) (extracellular domain) affinity | Human enzyme | Biolayer interferometry assay | Kd |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | BT474 human breast ductal carcinoma cells (HER2 [ERBB2]-overexpressing) | Fluorescent-activated cell sorting (FACS) assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | CAPAN1 human pancreas adenocarcinoma cells | Flow cytometry assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | CAPAN1 human pancreas adenocarcinoma cells (HER2 [ERBB2]-expressing) | Fluorescent-activated cell sorting (FACS) assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | CHO Chinese hamster ovary cells transfected with human enzyme | Flow cytometry assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | HCC1954 human breast ductal carcinoma cells | Flow cytometry assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | Human enzyme | Kd | |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | JIMT1 human breast carcinoma cells | Flow cytometry assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | JIMT1 human breast carcinoma cells (HER2 [ERBB2]-overexpressing) | Fluorescent-activated cell sorting (FACS) assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | MCF7 human breast adenocarcinoma cells (hormone-dependent) (HER2 [ERBB2] low-expressing) | Fluorescent-activated cell sorting (FACS) assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | N87 human gastric carcinoma cells | Flow cytometry assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | N87 human gastric carcinoma cells (HER2 [ERBB2]-overexpressing) | Fluorescent-activated cell sorting (FACS) assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | Recombinant cynomolgus monkey enzyme | Biolayer interferometry assay | Kd |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | Recombinant human enzyme | Biolayer interferometry assay | Kd |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | Recombinant human enzyme | ELISA assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | SKBr3 human breast adenocarcinoma cells (HER2 [ERBB2]-overexpressing) | Fluorescent-activated cell sorting (FACS) assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | SKOV3 human ovary adenocarcinoma cells | Flow cytometry assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | Surface plasmon resonance assay | Kd | |
Protein-tyrosine kinase (HER2 [ErbB2]) affinity | Kd | ||
Protein-tyrosine kinase (HER2 [ErbB2]) expression, induction | Calu3 human lung carcinoma cells (HER2 [ERBB2]-overexpressing) | MEC | |
Protein-tyrosine kinase (HER2 [ErbB2]) expression, induction | NCI-H2170 human non-small-cell lung cancer cells (HER2 [ERBB2] amplification-expressing) | MEC | |
Protein-tyrosine kinase (HER2 [ErbB2]) phosphorylation, induction | MDAMB453 human breast carcinoma cells | Chemiluminescent assay | MEC |
Protein-tyrosine kinase (HER2 [ErbB2]) phosphorylation, inhibition | MDAMB453 human breast carcinoma cells (HER2 [ERBB2]-overexpressing) | Chemiluminescent assay | MIC |
Protein-tyrosine kinase (HER2 [ErbB2]) phosphorylation, inhibition | SKBr3 human breast adenocarcinoma cells (HER2 [ERBB2]-overexpressing) | Chemiluminescent assay | MIC |
Protein-tyrosine kinase (HER2 [ErbB2]), inhibition | Purified enzyme | IC-50 | |
Protein-tyrosine kinase (HER2 [ErbB2]), inhibition | Recombinant enzyme | Fluorescence resonance energy transfer (FRET) assay | IC-50 |
Protein-tyrosine kinase (HER2 [ErbB2]), inhibition | IC-50 |
Fms Related Receptor Tyrosine Kinase 3 (FLT3) plays a crucial role in bladder cancer progression by promoting cell proliferation and survival. FLT3 testing is vital for identifying potential drug candidates and understanding drug efficacy. We offer FLT3 activity measurement using chemiluminescent, fluorescent, ATP, and ELISA assays, employing Poly(L-alanine/L-glutamic acid/L-lysine/L-tyrosine) as substrate. The main parameter assessed is IC-50, enabling accurate evaluation of inhibitor potency.
Pharmacological Activity | Material | Method | Parameter |
---|---|---|---|
Protein-tyrosine kinase (FLT3) (D835Y-mutated), inhibition | IC-50 | ||
Protein-tyrosine kinase (FLT3), inhibition | ATP assay | IC-50 | |
Protein-tyrosine kinase (FLT3), inhibition | Chemiluminescent assay | IC-50 | |
Protein-tyrosine kinase (FLT3), inhibition | ELISA assay | IC-50 | |
Protein-tyrosine kinase (FLT3), inhibition | Fluorescent assay | IC-50 | |
Protein-tyrosine kinase (FLT3), inhibition | IC-50 | ||
Protein-tyrosine kinase (FLT3-ITD), inhibition | Recombinant human enzyme | Poly(L-alanine/L-glutamic acid/L-lysine/L-tyrosine) as substrate | IC-50 |
Protein-tyrosine kinase (FLT3-ITD), inhibition | IC-50 |
Kit Proto-Oncogene, Receptor Tyrosine Kinase (KIT) plays a crucial role in bladder cancer progression by regulating cell growth and survival. Testing KIT activity is vital for developing targeted therapies. Our service utilizes ELISA and ATP assays to accurately measure KIT function and inhibitor efficacy, with IC-50 determination as the main parameter for drug candidate evaluation, ensuring precise assessment of potential therapeutic compounds.
Pharmacological Activity | Material | Method | Parameter |
---|---|---|---|
Protein-tyrosine kinase (c-Kit), inhibition | Recombinant human enzyme | ATP assay | IC-50 |
Protein-tyrosine kinase (c-Kit), inhibition | Recombinant human enzyme | IC-50 | |
Protein-tyrosine kinase (c-Kit), inhibition | ELISA assay | IC-50 | |
Protein-tyrosine kinase (c-Kit), inhibition | IC-50 |
Receptor Interacting Serine/Threonine Kinase 2 (RIPK2) is implicated in inflammation and tumor progression in bladder cancer. Testing RIPK2 activity is crucial for identifying and evaluating novel therapeutics. Our service utilizes sensitive chemiluminescent and ATP assays to measure kinase inhibition, providing precise IC-50 values. This enables rapid and accurate assessment of drug candidates targeting RIPK2, accelerating bladder cancer drug development.
Pharmacological Activity | Material | Method | Parameter |
---|---|---|---|
Serine/threonine protein kinase (RIPK2), inhibition | Recombinant enzyme | Chemiluminescent assay | IC-50 |
Serine/threonine protein kinase (RIPK2), inhibition | Recombinant human enzyme | ATP assay | IC-50 |
Serine/threonine protein kinase (RIPK2), inhibition | IC-50 |
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Experimental Scheme
Implementation
Conclusion