MET kinase-IN-2

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MET kinase-IN-2 

MET kinase-IN-2 是一种有效的选择性的，具有口服活性的 MET 激酶抑制剂，IC50 值为 7.4 nM。MET kinase-IN-2 具有抗肿瘤活性。

MET kinase-IN-2

MET kinase-IN-2 Chemical Structure

CAS No. : 2101241-90-9

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生物活性

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].

IC50 & Target[1]

MET

7.4 nM (IC50)

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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).

分子量

562.59

Formula

C33H27FN4O4
CAS 号

2101241-90-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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