JH-VIII-157-02,99.67%

产品编号:Bellancom-112140| CAS NO:1639422-97-1| 分子式:C28H27N5O2| 分子量:465.55

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-112140
5100.00 杭州 北京(现货)
Bellancom-112140
8150.00 杭州 北京(现货)
Bellancom-112140
15500.00 杭州 北京(现货)

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JH-VIII-157-02

产品介绍 JH-VIII-157-02 是 alectinib 的结构类似物,为 ALK 抑制剂,对棘皮动物微管相关蛋白样 4 (EML4)-ALK G1202R 的 IC50 值为 2 nM。
生物活性

JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.

体外研究

JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells. JH-VIII-157-02 also potently inhibits EML4-ALKwt (Eawt), EAC1156Y, EAF1174L, EAS1206Y (IC50, 2 nM), EAG1269A (IC50, 3 nM), EAL1196M (IC50, 58 nM), EA1151Tins (IC50, 107 nM), and EAL1152R (IC50, 196 nM). Moreover, JH-VIII-157-02 has selectivity at other kinases, including IRAK1, CLK4, RET, RET V804L, RET V804M and IRAK 4, and the IC50s are 14 nM, 14 nM, 3 nM, 13 nM, 12 nM, and 465 nM respectively. JH-VIII-157-02 exhibits inhibitory growth of cancer cell lines, such as H3122, DFCI76 (L1152R] with EC50s of 5, 19 nM, respectively.

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

体内研究

JH-VIII-157-02 exhibits good oral bioavailability following an oral dose of 10 mg/kg in mice. JH-VIII-157-02 also penetrates the CNS of mice.

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

体内研究

JH-VIII-157-02 exhibits good oral bioavailability following an oral dose of 10 mg/kg in mice. JH-VIII-157-02 also penetrates the CNS of mice.

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 : ≥ 25 mg/mL (53.70 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1480 mL 10.7400 mL 21.4800 mL
5 mM 0.4296 mL 2.1480 mL 4.2960 mL
10 mM 0.2148 mL 1.0740 mL 2.1480 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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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