Capmatinib (INCB28060) is a potent, orally available selective inhibitor of the c-MET receptor tyrosine kinase, a clinically validated cancer target. Capmatinib (INCB28060) exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10,000-fold selectivity over a large panel of human kinases. INCB28060 potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines. Capmatinib (INCB28060) potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis in vitro. Oral dosing of INCB28060 results in time- and dose-dependent inhibition of c-MET phosphorylation and tumor growth in c-MET-driven mouse tumor models, and INCB28060 is well tolerated at doses that achieve complete tumor inhibition.
Mol Cancer Ther. 2017 Nov;16(11):2399-2409.
Dual inhibition of Hedgehog and c-Met pathways for pancreatic cancer treatment
Capmatinib (INCB28060) purchased from AbMole
Cancer Res. 2017 Jan 1;77(1):41-52.
Heterogeneous Stromal Signaling within the Tumor Microenvironment Controls the Metastasis of Pancreatic Cancer
Capmatinib (INCB28060) purchased from AbMole
Nature. 2015 Jun 18;522(7556):349-53.
MET is required for the recruitment of anti-tumoural neutrophils.
Capmatinib (INCB28060) purchased from AbMole
Cell Experiment | |
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Cell lines | SUN-5 and SUN-1 cells |
Preparation method | Optimal cell density used in the viability assay was predetermined for individual cell lines. To determine compound potency, cells were seeded into 96-well microplates at the appropriate density in media containing 1% to 2% FBS and supplemented with serial dilutions of INCB28060 in a final volume of 100 μL per well. After 72-hour incubation, 24 μL of CellTiter 96 AQueous One Solution (Promega) was added to each well, and the plates were incubated for 2 hours in a 37°C incubator. The optical density was measured in the linear range using a microplate reader at 490 nm with wavelength correction at 650 nm. IC50 values were calculated using the GraphPad Prism Software. |
Concentrations | 0~333 nM |
Incubation time | 3 days |
Animal Experiment | |
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Animal models | B16F10 tumour-bearing mice |
Formulation | 0.5% methylcellulose in saline |
Dosages | 50mg/kg INCB28060 |
Administration | via oral gavage every day once a day starting from day 2 after tumour injection and twice a day from day 11 until the end of the experiment(2 weeks) |
Molecular Weight | 412.42 |
Formula | C23H17FN6O |
CAS Number | 1029712-80-8 |
Solubility (25°C) | DMSO 15 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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SAR125844 is a potent intravenously active and highly selective MET kinase inhibitor, displaying nanomolar activity against the wild-type kinase (IC50 value of 4.2 nmol/L) and H1094Y, Y1235D, M1250T, L1195V, and D1228H kinase domain mutants (IC50 values of 0.22, 1.7, 6.5, 65, and 81 nmol/L, respectively). |
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