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Capmatinib

Catalog No. T1963 CAS 1029712-80-8

Synonyms: NVP-INC280, INC-280, INCB28060

Capmatinib (INCB28060) is an orally bioavailable inhibitor of the proto-oncogene c-Met (HGFR)with potential antineoplastic activity.

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Capmatinib, CAS 1029712-80-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 61.00
25 mg	In stock	$ 75.00
50 mg	In stock	$ 97.00
100 mg	In stock	$ 133.00
200 mg	In stock	$ 169.00
500 mg	In stock	$ 283.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.76%

Purity: 98.94%

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Description	Capmatinib (INCB28060) is an orally bioavailable inhibitor of the proto-oncogene c-Met (HGFR)with potential antineoplastic activity.
Targets&IC50	c-Met:0.13 nM
In vitro	In a c-MET-dependent mouse tumor model, the oral administration of INCB28060 (0.03 mg/kg) effectively inhibited tumor growth.
In vivo	In tumor cells, INCB28060 inhibits cell proliferation and survival by downregulating c-MET phosphorylation and the signaling pathways mediated by c-MET.
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	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.(Only for Reference)

Synonyms	NVP-INC280, INC-280, INCB28060
Molecular Weight	412.42
Formula	C23H17FN6O
CAS No.	1029712-80-8

Storage

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

Solubility Information

DMSO: 4.12 mg/mL (10 mM), Sonification is recommended

References and Literature

1. Liu X, et al, Clin Cancer Res, 2011, 17(227). 7127-7138. 2. Cao Shangtao, Shengyong Yu, Dongwei Li, Jing Ye, Xuejie Yang, Chen Li, Xiaoshan Wang et al. Chromatin accessibility dynamics during chemical induction of pluripotency[J]. Cell stem cell. 2018 Apr 22(4): 529-542. e5.

Citations

1. Cao Shangtao, Shengyong Yu, Dongwei Li, Jing Ye, Xuejie Yang, Chen Li, Xiaoshan Wang et al. Chromatin accessibility dynamics during chemical induction of pluripotency. Cell Stem Cell. 2018, 22(4): 529-542. e5 2. Jiao D, Chen Y, Liu X, et al.Targeting MET endocytosis or degradation to overcome HGF-induced gefitinib resistance in EGFR-sensitive mutant lung adenocarcinoma.Biochemical and Biophysical Research Communications.2023 3. Tang J, Qi C, Bai X, et al.Cell Membrane-Anchored DNA Nanoinhibitor for Inhibition of Receptor Tyrosine Kinase Signaling Pathways via Steric Hindrance and Lysosome-Induced Protein Degradation.ACS Pharmacology & Translational Science.2023

Related compound libraries

This product is contained In the following compound libraries：

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

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Keywords

Capmatinib 1029712-80-8 Apoptosis Tyrosine Kinase/Adaptors c-Met/HGFR orally active NVP-INC280 ATP competitive H441 Balb/c nu/nu mice NVP-INC-280 inhibit INC 280 Inhibitor INC-280 INC280 SNU-5 INCB 28060 NVP-INC 280 U-87MG INCB28060 INCB-28060 S114 inhibitor

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