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首页-小分子抑制剂&激动剂-Tyrosine Kinase-TAM Receptor (Tyro3-Axl-Mer)-DS-1205b
DS-1205b

Chemical Structure : DS-1205b

CAS No.: 1855860-24-0

DS-1205b (DS1205b)

货号: PC-38043Not For Human Use, Lab Use Only.

DS-1205b (DS1205b) is a potent, highly selective inhibitor of AXL kinase with IC50 of 1.3 nM.

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

生物&药学活性

DS-1205b (DS1205b) is a potent, highly selective inhibitor of AXL kinase with IC50 of 1.3 nM.
DS-1205b displays 48-, 80-, and 313-fold selectivity ovver MER, MET, and TRKA.
DS-1205b inhibits phosphorylation of AKT serine/threonine kinase in a dose-dependent manner.
DS-1205b does not obviously inhibit cell proliferation and viability in NIH3T3-AXL cells.
DS-1205b significantly suppresses cell migration on NIH3T3-AXL with IC50 of 2.7 nM.
DS-1205b induces tumor regression by 54-86% at doses of 6.3-50 mg/kg in mice bearing subcutaneously implanted NIH3T3-AXL cells.
DS-1205b inhibits AXL signaling in vitro when combined with erlotinib or osimertinib, delays erlotinib acquired resistance and restores the treatment effect of erlotinib in an HCC827 sc xenograft model.

物理化学性质&存储条件

分子量 735.81
分子式 C41H42FN5O7
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

(R)-N-(4-(5-(4-((1,4-dioxan-2-yl)methoxy)-3-methoxyphenyl)-2-aminopyridin-3-yl)-3-fluorophenyl)-5-methyl-4'-oxo-1'-((tetrahydro-2H-pyran-4-yl)methyl)-1',4'-dihydro-[2,3'-bipyridine]-5'-carboxamide

参考文献

1. Takeshi Jimbo, et al. Oncotarget. 2019 Aug 27;10(50):5152-5167.

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