ChemicalBook CAS DataBase List 1029712-80-8

1029712-80-8

Name	INCB28060
CAS	1029712-80-8
EINECS(EC#)	813-241-9
Molecular Formula	C23H17FN6O
MDL Number	MFCD18633285
Molecular Weight	412.419
MOL File	1029712-80-8.mol

Synonyms

NC280 INC280 CS-192 INC28060 INCB28060 NVP-INC280 INCB028060 CapMatinib BenzaMide HCl Capmatinib base INCB28060, INC280 INC280 Capmatinib CAPMATINIB (INC280) BenzaMide INCB28060 INC 280 (INCB28060) INCB28060,BenzaMide Capmatinib USP/EP/BP INCB28060(Capmatinib) CapMatinib (INCB28060) INCB 28060; INCB-28060; INC280 CAPMATINIB (INCB28060);INCB-28060; INC-280 2-Fluoro-N-methyl-4-[7-(6-quinolinylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide 2-Fluoro-N-Methyl-4-(7-quinolin-6-ylMethyl-iMidazo[1,2-b][1,2,4] triazin-2-yl)-benzaMide BenzaMide, 2-fluoro-N-Methyl-4-[7-(6-quinolinylMethyl)iMidazo[1,2-b][1,2,4]triazin-2-yl]- NC280 BenzaMide,2-fluoro-N-Methyl-4-[7-(6-quinolinylMethyl)iMidazo[1,2-b][1,2,4]triazin-2-yl]- BenzaMide, 2-fluoro-N-Methyl-4-[7-(6-quinolinylMethyl)iMidazo[1,2-b][1,2,4]triazin-2-yl]- INCB28060 INC28060(BenzaMide, 2-fluoro-N-Methyl-4-[7-(6-quinolinylMethyl)iMidazo[1,2-b][1,2,4]triazin-2-yl]-) 2-fluoro-n-methyl-4-[7-[(quinolin-6-yl)methyl]imidazo[1,2-b]-[1,2,4]triazin-2-yl]benzamide capmatinib 2-Fluoro-N-methyl-4-[7-[(quinolin-6-yl)methyl]imidazo[1,2-b]-[1,2,4]triazin-2-yl]benzamide Capmatinib (INCB28060)

Chemical Properties

Melting point	>250°C (dec.)
density	1.40
vapor pressure	0-0Pa at 20-25℃
storage temp.	-20°C Freezer, Under inert atmosphere
solubility	DMSO (Slightly), Methanol (Slightly)
form	Solid
pka	13.82±0.46(Predicted)
color	Pale Yellow to Light Yellow
InChI	InChI=1S/C23H17FN6O/c1-25-22(31)18-6-5-16(11-19(18)24)21-13-28-23-27-12-17(30(23)29-21)10-14-4-7-20-15(9-14)3-2-8-26-20/h2-9,11-13H,10H2,1H3,(H,25,31)
InChIKey	LIOLIMKSCNQPLV-UHFFFAOYSA-N
SMILES	C(NC)(=O)C1=CC=C(C2=NN3C(CC4=CC=C5C(=C4)C=CC=N5)=CN=C3N=C2)C=C1F
LogP	1.6-2.2 at 35℃ and pH7-9

Hazard Information

Description

Capmatinib is a competitive inhibitor with very potent and selective activity against MET compared to other kinases.

Uses

2-Fluoro-N-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzamide is used in the preparation of a combination formulation with allosteric SHP2 inhibitor TNO155. Used in treatment of non-small cell lung cancer with specific mutations (those that lead to mesenchymal-epithelial transition or MET exon 14 skipping).

Side effects

Most common adverse events were nausea, peripheral edema, decreased appetite, rash, and increased amylase and lipase levels.

in vitro

It has been shown in vitro that cell lines made resistant to erlotinib, an EGFR inhibitor, could be resensitized after capmatinib treatment. Results from a phase Ib/II study of patients with EGFR-mutated, MET-dysregulated NSCLC have shown promising responses to a combination of capmatinib and gefitinib (EGFR TKI) following disease progression from an only EGFR TKI treatment regimen. Recommended phase II dose was determined to be capmatinib 400 mg twice/day and gefitinib 250 mg once/day.

target

c-MET

Dosage

The recommended capmatinib dose is 400 mg orally twice daily with or without food.

References

1. liu x, wang q, yang g, et al. a novel kinase inhibitor, incb28060, blocks c-met-dependent signaling, neoplastic activities, and cross-talk with egfr and her-3. clinical cancer research : an official journal of the american association for cancer research. 2011;17(22):7127-7138.

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