MET kinase-IN-2

Modify Date: 2024-01-02 16:46:06

MET kinase-IN-2 structure	Common Name	MET kinase-IN-2
	CAS Number	2101241-90-9	Molecular Weight	562.59
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₃₃H₂₇FN₄O₄	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of MET kinase-IN-2

MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity[1].

Name	MET kinase-IN-2

Description	MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR
Target	MET:7.4 nM (IC50)
In Vitro	MET kinase-IN-2 (compound 20j; 72 hours) inhibits U-87 MG, NIH-H460, HT-29, and MKN-45 cell lines with IC50s ranging 2.9 to 4.5 μM[1]. MET kinase-IN-2 inhibits AXL, Flt4, KDR, Mer, TEK, and TYRO3 with IC50s ranging from 16.5 to 198 nM[1].
In Vivo	MET kinase-IN-2 (3-37.5 mg/kg; p.o.; 7 days per week for 3 weeks) exhibits statistically significant tumor growth inhibition in the U-87 MG 24 xeograft model[1]. MET kinase-IN-2 treatment shows that the Cmax, AUC0-∞, T1/2，CL, and F% values are 1.5 µg/mL, 10.7 µg•h/mL, 4.9 hours, 0.5 L/h/kg, and F=32%, respectively[1]. Animal Model: 4-6 weeks old Female nude mice (U-87 MG xenograft model)[1] Dosage: 3, 6, 12.5, 37.5 mg/kg Administration: P.o.; 7 days per week for 3 weeks Result: Induced dose-dependent tumor growth inhibition. Animal Model: Male SD rats[1] Dosage: 5 mg/kg Administration: P.o. (Pharmacokinetic Analysis) Result: Displayed favorable overall PK profiles, with maximal plasma concentration (Cmax=1.5 µg/mL, 5-fold higher to that of IV), plasma exposure (AUC0-∞=10.7 µg•h/mL, 9.7-fold higher to that of IV), half-life (T1/2=4.9 h, 4.9-fold longer to that of IV), total clearance CL (0.5 L/h/kg; 10-fold lower to that of IV), and oral bioavailability (F=32%, 2.7-fold higher to that of IV) after oral dose of 5 mg/kg (10 mg/kg for IV).
References	[1]. Chen T, et al. Discovery of 1,6-naphthyridinone-based MET kinase inhibitor bearing quinoline moiety as promising antitumor drug candidate. Eur J Med Chem. 2020;192:112174.

Molecular Formula	C₃₃H₂₇FN₄O₄
Molecular Weight	562.59