Capmatinib

Bezeichnung:Capmatinib

CAS-Nr1029712-80-8

Englisch Name:Capmatinib

CBNumberCB92574678

SummenformelC23H17FN6O

Molgewicht412.42

MOL-Datei1029712-80-8.mol

Capmatinib physikalisch-chemischer Eigenschaften

Schmelzpunkt	>250°C (dec.)
Dichte	1.40
Dampfdruck	0-0Pa at 20-25℃
storage temp.	-20°C Freezer, Under inert atmosphere
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
pka	13.82±0.46(Predicted)
Aggregatzustand	Solid
Farbe	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

Gefahreninformationscode (GHS)

Capmatinib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
INCB 28060 is an inhibitor of heptatocyte growth factor receptor (HGFR, also known as c-Met), potently blocking in vitro kinase activity (IC₅₀ = 0.13 nM) as well as constitutive or HGF-stimulated activity in cells (IC₅₀ values range from 0.3 to 1.1 nM). It blocks cell proliferation and migration or induces apoptosis in different types of cancer cells. INCB 28060 is orally bioavailable and inhibits the growth of HGFR-dependent tumors in mice. It also improves efficacy of gemcitabine in a mouse pancreatic cancer model and reduces migration and adhesion in ovarian cancer cell models.
Beschreibung
Capmatinib is a competitive inhibitor with very potent and selective activity against MET compared to other kinases.
Verwenden
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).
Trademarks
Tabrecta
Allgemeine Beschreibung
Class: receptor tyrosine kinase; Treatment: NSCLC with METex14; Other name: INCB28060; Oral bioavailability >70%; Elimination half-life = 7.8 h; Protein binding = 96%
Nebenwirkungen
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
Einzelnachweise
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.

Capmatinib Upstream-Materialien And Downstream Produkte

Capmatinib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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