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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Src-Bosutinib
Bosutinib

Chemical Structure : Bosutinib

CAS No.: 380843-75-4

Bosutinib (SKI-606, SKI 606)

货号: PC-24042Not For Human Use, Lab Use Only.

Bosutinib (SKI-606) is a potent, dual Src/Abl inhibitor with IC50 of 1.2 nM (Src enzyme), inhibits Src autophosphorylation with an IC50 of 0.25 uM in HT29 cells, inhibits bacterially expressed Abl kinase activity with IC50 of 1 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Bosutinib (SKI-606) is a potent, dual Src/Abl inhibitor with IC50 of 1.2 nM (Src enzyme), inhibits Src autophosphorylation with an IC50 of 0.25 uM in HT29 cells, inhibits bacterially expressed Abl kinase activity with IC50 of 1 nM.
Bosutinib (SKI-606) inhibits the growth of the Abl-MLV-transformed fibroblasts with IC50 of 90 nM
Bosutinib (SKI-606) inhibits v-Abl phosphorylation with IC50 of 25-50 nM, inhibits STAT5 Phosphorylation.
Bosutinib (SKI-606) inhibits anchorage-independent growth of Src-transformed fibroblasts with an IC50 of 100 nM, and inhibits Src-dependent protein tyrosine phosphorylation.
Bosutinib (SKI-606) inhibits proliferation in CML cells, inhibits tyrosine phosphorylation of cellular proteins and Bcr-Abl in CML cells.
Bosutinib (SKI-606) displays excellent antitumor activity in Src-transformed fibroblast xenografts in nude mice.

物理化学性质&存储条件

分子量 530.45
分子式 C26H29Cl2N5O3
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

4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

参考文献

1. Golas JM, et al. Cancer Res. 2003 Jan 15;63(2):375-81.

2. Golas JM, et al. Cancer Res. 2005 Jun 15;65(12):5358-64.

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