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首页-小分子抑制剂&激动剂-Tyrosine Kinase-IGF-1R-GSK1838705A
GSK1838705A

Chemical Structure : GSK1838705A

CAS No.: 1116235-97-2

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GSK1838705A (GSK 1838705A;GSK-1838705A)

货号: PC-43330Not For Human Use, Lab Use Only.

GSK1838705A is a potent, specific inhibitor of IGF-IR and insulin receptor (IR) with IC50 of 2.0 and 1.6 nM, also is a potent inhibitor of ALK with IC50 of 0.5 nM.

规格 价格 库存 数量
10 mg ￥1480 In stock
25 mg ￥2580 In stock
50 mg ￥4280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK1838705A is a potent, specific inhibitor of IGF-IR and insulin receptor (IR) with IC50 of 2.0 and 1.6 nM, also is a potent inhibitor of ALK with IC50 of 0.5 nM.
GSK1838705A display excellent kinase selectivity on a panel of 224 unique protein kinases with only 7 additional kinases to be inhibited by >50% at 0.3 uM.
GSK1838705A inhibits a panel of cell lines derived from solid and hematologic tumors with IC50 of 20 nM-8 uM (NCI-H929 IC50=197 nM).
GSK1838705A causes complete regression of ALK-dependent tumors, retards the growth of human tumor xenografts in vivo with minimal effects on glucose homeostasis.

物理化学性质&存储条件

分子量 532.5693
分子式 C27H29FN8O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

Benzamide, 2-[[2-[[1-[2-(dimethylamino)acetyl]-2,3-dihydro-5-methoxy-1H-indol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methyl-

参考文献

1. Sabbatini P, et al. Mol Cancer Ther. 2009 Oct;8(10):2811-20.

2. Zhou F, et al. Onco Targets Ther. 2015 Apr 10;8:753-60.

3. Refolo MG, et al. Oncotarget. 2017 Sep 30;8(61):103465-103476.

4. Kelleher FC, et al. Eur J Cancer. 2010 Sep;46(13):2357-68.

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