4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
产品详情
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。
生物活性
MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC 50 of 7.4 nM. MET kinase-IN-2 has antitumor activity.
性状
Solid
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.MET kinase-IN-2 inhibits AXL, Flt4, KDR, Mer, TEK, and TYRO3 with IC50s ranging from 16.5 to 198 nM. 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.
MET kinase-IN-2 treatment shows that the C max , AUC 0-∞ , T 1/2 ,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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (177.75 mM; Need ultrasonic)配制储备液