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Capmatinib 2HCl

Catalog No. T4260 CAS 1197376-85-4

Synonyms: INC-280 2HCl, INCB28060 2HCl

Capmatinib 2HCl (INC-280 2HCl) is a novel, ATP-competitive inhibitor of c-MET kinase with an IC50 with 0.13 nM.Capmatinib 2HCl 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. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines. As a result, Capmatinib 2HCl potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis in vitro.

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Capmatinib 2HCl, CAS 1197376-85-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 37.00
2 mg	In stock	$ 50.00
5 mg	In stock	$ 64.00
10 mg	In stock	$ 79.00
25 mg	In stock	$ 148.00
50 mg	In stock	$ 271.00
100 mg	In stock	$ 453.00
500 mg	In stock	$ 1,050.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 100%

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Description	Capmatinib 2HCl (INC-280 2HCl) is a novel, ATP-competitive inhibitor of c-MET kinase with an IC50 with 0.13 nM.Capmatinib 2HCl 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. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines. As a result, Capmatinib 2HCl potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis in vitro.
Targets&IC50	c-Met (cell-free assay):0.13 nM
In vitro	INCB28060(free base）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 inhibits human c-MET phosphorylation and c-MET-mediated signaling in cancer cells. INCB28060 inhibits c-MET-dependent cell proliferation and survival, and prevents anchorage-independent cancer cell growth and cell migration.
In vivo	INCB28060(free base) shows strong antitumor activity in c-MET-dependent mouse tumor models, even oral treatment of 0.03 mg/kg INCB28060 causes approximately 50% inhibition of c-MET-phosphorylation. Dose-dependent inhibition of tumor growth is observed in tumor-bearing mice.
Kinase Assay	c-Met Kinase Assay:The assay buffer contains 50 mM Tris-HCl, 10 mM MgCl2, 100 mM NaCl, 0.1 mg/ml BSA, 5 mM DTT, pH 7.8. For HTS 0.8 μL of 5 mM of INCB28060 dissolved in DMSO are dotted on 384-well plates. DMSO titration suggests that the maximum tolerated concentration of the solvent is 4%. To measure IC50s the INCB28060 plate is prepared by 3-fold and 11-point serial dilutions. 0.8 μL of INCB28060 in DMSO is transferred from INCB28060 plate to the assay plate. The final concentration of DMSO is 2%. Solutions of 8 nM unphosphorylated c-Met or 0.5 nM phosphorylated c-Met are prepared in assay buffer. A 1 mM stock solution of peptide substrate Biotin-EQEDEPEGDYFEWLE-amide dissolved in DMSO is diluted to 1 μM in assay buffer containing 400 μM ATP (unphosphorylated c-Met) or 160 uM ATP (phosphorylated c-Met). A 20 μL volume of enzyme solution (or assay buffer for the enzyme blank) is added to the appropriate wells in each plate and then 20 μL/well of substrate solution to initiate the reaction. The plate is protected from light and incubated at 25 °C for 90 minutes. The reaction is stopped by adding 20 μL of a solution containing 45 mM EDTA, 50 mM Tris-HCl, 50 mM NaCl, 0.4 mg/ml BSA, 200 nM SA-APC and 3 nM EUPy20. The plate is incubated for 15-30 minutes at room temperature and HTRF (homogenous time resolved fluorescence) is measured on a Perkin Elmer Fusion α-FP instrument. The HTRF program settings used are as follows: Primary excitation filter 330/30, Primary window: 200 uSec, Primary delay: 50 uSec, Number of flashes: 15, Well read time: 2000
Cell Research	Cell lines: H441 cells. Concentrations: 0.24,1,4,16,63 nM. Incubation Time: 24 hours. Method:H441 cells are seeded in RPMI-1640 medium containing 10% FBS and grown to complete confluence.Gaps are introduced by scraping cells with a P200 pipette tip.Cells are then stimulated with 50 ng/mL recombinant human HGF to induce migration across the gap in the presence of various concentrations of INCB28060.After an overnight incubation,representative photographs are taken and a semiqualitative assessment of inhibition of cell migration is conducted.
Animal Research	Animal Models: Eight-week-old female Balb/c nu/nu mice (Charles River) are inoculated subcutaneously with 4 × 106 tumor cells (S114 model) or with 5 × 106 tumor cells (U-87 mg glioblastoma model). Formulation: INCB28060 is prepared as a 5 mM stock solution in 100% dimethyl sulfoxide and routinely stored at room temperature. Dosages: 3,10,30 mg/kg. Administration: INCB28060 is orally dosed,twice each day.

Synonyms	INC-280 2HCl, INCB28060 2HCl
Molecular Weight	485.34
Formula	C23H19Cl2FN6O
CAS No.	1197376-85-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 11 mg/mL (22.66 mM)

References and Literature

1. Liu X, et al,A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3. Clin Cancer Res, 2011, 17(227). 7127-7138.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library FDA-Approved Kinase Inhibitor Library EMA Approved Drug Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library

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Antitumor agent-111 AMG-337 SGX-523 Hepln-13 Altiratinib BMS-2 Emibetuzumab MET/PDGFRA-IN-1

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Keywords

Capmatinib 2HCl 1197376-85-4 Tyrosine Kinase/Adaptors c-Met/HGFR Apoptosis H441 orally active SNU-5 INCB28060 Inhibitor INCB 28060 S114 INC280 INC-280 2HCl inhibit INC 280 Capmatinib INCB-28060 U-87MG ATP competitive INC-280 INCB28060 2HCl Balb/c nu/nu mice inhibitor

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