GSK-114|GSK-114|cas:1301761-96-5|西域试剂

GSK-114,GSK-114,98.08%

产品编号：Bellancom-117658| CAS NO：1301761-96-5| 分子式：C₁₉H₂₃N₅O₄S| 分子量：417.48

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货号	价格	库存与货期
Bellancom-117658	￥1800.00	杭州北京（现货）
Bellancom-117658	￥2700.00	杭州北京（现货）
Bellancom-117658	￥5700.00	杭州北京（现货）
Bellancom-117658	￥9700.00	杭州北京（现货）
Bellancom-117658	￥16500.00	杭州北京（现货）

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GSK-114

产品介绍

GSK-114 是一种高选择性的，具有口服活性的 TNNI3K 抑制剂 (IC₅₀= 25 nM)。GSK-114 对 TNNI3K 的选择性是 B-Raf 激酶的 40 倍 (IC₅₀= 1 µM)。TNNI3K(又称 CARK) 是酪氨酸样激酶家族的成员，在心脏组织中选择性表达。

生物活性

GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC₅₀= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC₅₀= 1 µM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue.

体外研究

At a concentration of 1 µM, GSK114 demonstrated an affinity for seven other kinases: ACK1, B-Raf, GAK, MEK5, PDGFRB, STK36, and ZAK.

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

体内研究

GSK-114 affords the best balance of specificity and pharmacokinetics, demonstrating useful oral exposure (poDNAUC=0.18, C_max=130 ng/ml @ 2 mg/kg, t_1/2=3.6 hr, rat F_u=20.2%).

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

体内研究

GSK-114 affords the best balance of specificity and pharmacokinetics, demonstrating useful oral exposure (poDNAUC=0.18, C_max=130 ng/ml @ 2 mg/kg, t_1/2=3.6 hr, rat F_u=20.2%).

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 5.95 mg/mL (14.25 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3953 mL	11.9766 mL	23.9532 mL
5 mM	0.4791 mL	2.3953 mL	4.7906 mL
10 mM	0.2395 mL	1.1977 mL	2.3953 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。-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