MET kinase-IN-2|cas:2101241-90-9|西域试剂

MET kinase-IN-2,98.39%

产品编号：Bellancom-131065| CAS NO：2101241-90-9| 分子式：C₃₃H₂₇FN₄O₄| 分子量：562.59

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货号	价格	库存与货期
Bellancom-131065	￥2100.00	杭州北京（现货）
Bellancom-131065	￥3370.00	杭州北京（现货）
Bellancom-131065	￥6400.00	杭州北京（现货）
Bellancom-131065	￥10250.00	杭州北京（现货）

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MET kinase-IN-2

产品介绍

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 IC₅₀ of 7.4 nM. MET kinase-IN-2 has antitumor activity.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 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)
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
Dosage:	5 mg/kg
Administration:	P.o. (Pharmacokinetic Analysis)
Result:	Displayed favorable overall PK profiles, with maximal plasma concentration (C_max=1.5 µg/mL, 5-fold higher to that of IV), plasma exposure (AUC_0-∞=10.7 µg•h/mL, 9.7-fold higher to that of IV), half-life (T_1/2=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).

体内研究

西域 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)
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
Dosage:	5 mg/kg
Administration:	P.o. (Pharmacokinetic Analysis)
Result:	Displayed favorable overall PK profiles, with maximal plasma concentration (C_max=1.5 µg/mL, 5-fold higher to that of IV), plasma exposure (AUC_0-∞=10.7 µg•h/mL, 9.7-fold higher to that of IV), half-life (T_1/2=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).

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (177.75 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7775 mL	8.8875 mL	17.7749 mL
5 mM	0.3555 mL	1.7775 mL	3.5550 mL
10 mM	0.1777 mL	0.8887 mL	1.7775 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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