DS-1205b free base|1855860-24-0|-陌孚医药/Medlife

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DS-1205b free base

目录号: PL12417 纯度: ≥99%

CAS No. :1855860-24-0

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中文名称	DS-1205b free base
英文名称	DS-1205b free base
英文别名	DS-1205b free base;A937778;(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;N-[4-[2-amino-5-[4-[[(2R)-1,4-dioxan-2-yl]methoxy]-3-methoxyphenyl]pyridin-3-yl]-3-fluorophenyl]-5-(;BDBM531987;US11208403, Example 64;AT27659;DS-1205b (free base)
Cas No.	1855860-24-0
分子式	C₄₁H₄₂FN₅O₇
分子量	735.80
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	DS-1205b free base 是一种有效和选择性的 AXL 激酶抑制剂，IC₅₀ 值为 1.3 nM。DS-1205b free base 还可以抑制 MER，MET 和 TRKA，IC₅₀ 值分别为 63、104 和 407 nM。 DS-1205b free base 可以抑制细胞迁移和肿瘤生长。
生物活性	DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC 50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC 50 s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.
性状	Solid
IC50 & Target[1][2]	AXL 1.3 nM (IC50) MER 63 nM (IC50u
体外研究(In Vitro)	DS-1205b (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC50=2.7 nM). DS-1205b (1-10000 μM; 2-24 h) significantly inhibits the phosphorylation of AXL in NIH3T3-AXL cells. DS-1205b decreases NIH3T3 cell proliferation but not obviously inhibits growth (GI50>10,000 nM). has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
体内研究(In Vivo)	DS-1205b (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female NOD/Shi-scid IL-2Rγ KO Ji
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
参考文献	[1]. Jimbo T, et, al. DS-1205b, a novel selective inhibitor of AXL kinase, blocks resistance to EGFR-tyrosine kinase inhibitors in a non-small cell lung cancer xenograft model. Oncotarget. 2019 Aug 27;10(50):5152-5167.

溶解度数据	In Vitro: DMSO : 50 mg/mL (67.95 mM; Need ultrasonic)配制储备液

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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