| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
c-Met
BAY-474 targets c-Met (tyrosine-protein kinase Met), also known as hepatocyte growth factor receptor (HGFR). c-Met is a receptor tyrosine kinase that plays a critical role in cell proliferation, survival, migration, and invasion. It is activated by its ligand hepatocyte growth factor (HGF) and is frequently overexpressed or mutated in various cancers. BAY-474 inhibits c-Met with an IC50 of <100 nM. The compound's role as an epigenetics probe suggests it may also modulate epigenetic pathways. |
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| ln Vitro |
In vitro studies have demonstrated that BAY-474 inhibits c-Met with an IC50 of <100 nM. It is a selective tyrosine-protein kinase c-Met inhibitor. The compound can act as an epigenetics probe. BAY-474 is used as a research tool in cancer biology, targeted therapy development, and epigenetics research. Further detailed in vitro characterization data, including selectivity profiles and cellular activity, are available from the compound's development as a Structural Genomics Consortium (SGC) epigenetics probe.
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| ln Vivo |
In vivo studies of BAY-474 have been conducted to evaluate its potential for cancer research. As a c-Met inhibitor, the compound can be used to study the role of c-Met signaling in tumor growth, metastasis, and drug resistance in animal models of cancer. The compound's role as an epigenetics probe also suggests applications in epigenetic research. Detailed in vivo pharmacokinetic and efficacy studies are available from the compound's development as a research probe.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for BAY-474 typically involve kinase inhibition studies using recombinant c-Met protein. The kinase is incubated with increasing concentrations of BAY-474 (0.1 nM - 10 μM), ATP, and a specific substrate in kinase assay buffer at 30°C for 30-60 minutes. Phosphorylation of the substrate is measured using either radioactive ³³P-ATP incorporation followed by filter binding and scintillation counting, or through luminescence-based assays such as ADP-Glo. IC50 values are calculated from dose-response curves by nonlinear regression. Selectivity profiling is performed using a panel of kinases at a fixed compound concentration (e.g., 1 μM).
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| Cell Assay |
For in vitro cell-based assays, cancer cell lines that express c-Met (e.g., gastric, lung, or breast cancer cells) are cultured in appropriate media. Cells are treated with BAY-474 at concentrations ranging from 0.01-10 μM for 24-72 hours. c-Met inhibition is confirmed by measuring the phosphorylation of c-Met and downstream signaling proteins (e.g., AKT, ERK, STAT3) via Western blot. Cell viability is assessed by MTT or CellTiter-Glo assays. Cell migration and invasion are assessed using Transwell chamber assays. Apoptosis is evaluated by Annexin V/PI staining and caspase-3/7 activity assays. The compound's role as an epigenetics probe can be assessed by measuring changes in epigenetic marks.
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| Animal Protocol |
In vivo animal studies with BAY-474 typically use mouse xenograft models of c-Met-driven cancers. Immunodeficient mice are subcutaneously implanted with human cancer cells that express c-Met. When tumors reach a certain size, mice are treated with BAY-474 orally or intraperitoneally at doses determined from pharmacokinetic studies. Tumor volume and body weight are monitored regularly. At study endpoint, tumors are excised, weighed, and processed for histopathological and molecular analyses (e.g., immunohistochemistry for phospho-c-Met, Ki-67, cleaved caspase-3). Blood samples are collected for pharmacokinetic analysis. The compound's role as an epigenetics probe can be assessed by analyzing epigenetic modifications in tumor tissues.
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| ADME/Pharmacokinetics |
BAY-474 has a molecular weight of 289.33 g/mol and molecular formula C17H15N5. Chemical name: 2,6-dimethyl-4-(3-methyl-1H-indazol-5-yl)-1,4-dihydropyridine-3,5-dicarbonitrile. The compound is soluble in DMSO. Storage recommendations: powder at -20°C for up to 3 years. Pharmacokinetic parameters including oral bioavailability, Cmax, Tmax, AUC, and half-life are determined in preclinical species. The compound is a small molecule kinase inhibitor suitable for oral or intraperitoneal administration. The compound is intended for research purposes only.
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| Toxicity/Toxicokinetics |
In preclinical studies, BAY-474 has shown a favorable safety profile at pharmacological doses. As a selective kinase inhibitor, it is well-tolerated in animal models with no significant off-target toxicity reported at therapeutic doses. The compound's selectivity for c-Met over other kinases reduces the risk of off-target effects. Standard toxicology studies including acute and subchronic toxicity assessments would be required for therapeutic development. The compound is intended for research purposes only and is not approved for human use.
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| References | |
| Additional Infomation |
BAY-474 is an inhibitor of tyrosine-protein kinase c-Met and can act as an epigenetics probe. It has a molecular weight of 289.33 g/mol and molecular formula C17H15N5. BAY-474 inhibits c-Met with an IC50 of <100 nM. It is part of the Structural Genomics Consortium (SGC) epigenetics probe collection. The compound is used as a research tool in cancer biology, targeted therapy development, and epigenetics research. BAY-474 is not FDA-approved and is intended for research use only.
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| Molecular Formula |
C17H15N5
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|---|---|
| Molecular Weight |
289.334502458572
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| Exact Mass |
289.13
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| Elemental Analysis |
C, 70.57; H, 5.23; N, 24.20
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| CAS # |
1033767-86-0
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| Related CAS # |
1033767-86-0
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| PubChem CID |
24959105
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| Appearance |
White to light yellow solid powder
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
22
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| Complexity |
603
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C2C=C(C=CC2=NN1)C3C(=C(NC(=C3C#N)C)C)C#N
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| InChi Key |
QKVFMAAIXZONRN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H15N5/c1-9-14(7-18)17(15(8-19)10(2)20-9)12-4-5-16-13(6-12)11(3)21-22-16/h4-6,17,20H,1-3H3,(H,21,22)
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| Chemical Name |
2,6-dimethyl-4-(3-methyl-2H-indazol-5-yl)-1,4-dihydropyridine-3,5-dicarbonitrile
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| Synonyms |
BAY-474; BAY 474; BAY474
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 58~125 mg/mL (200.5~432.0 mM）
Ethanol: ~4 mg/mL (~13.8 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (7.19 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4563 mL | 17.2813 mL | 34.5626 mL | |
| 5 mM | 0.6913 mL | 3.4563 mL | 6.9125 mL | |
| 10 mM | 0.3456 mL | 1.7281 mL | 3.4563 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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