OSI-930|728033-96-3|(噻尔非尼)-陌孚医药/Medlife

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OSI-930 (Synonyms: 噻尔非尼)

目录号: PL01334 纯度: ≥98%

CAS No. :728033-96-3

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中文名称	OSI-930
中文别名	3-[(4-喹啉甲基)氨基]-N-[4-(三氟甲氧基)苯基]-2-噻吩甲酰胺;OSI930 抑制剂;OSI-930;噻尔非尼
英文名称	OSI-930
英文别名	OSI 930;OSI-930;3-(Quinolin-4-ylmethylamino)-N-(4-(trifluoromethoxy)phenyl)thiophene-2-carboxamide;3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide;3-((quinolin-4-ylmethyl)amino)-N-(4-(trifluoromethoxy)phenyl)th;3-[(quinolin-4-ylmethyl)amino]-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide;CHEMBL1614710;CID9868037;N-(4-trifluoromethoxyphenyl) 3-[(quinolin-4-ylmethyl)amino]thiophene-2-carboxamide;N-(4-trifluoromethoxyphenyl)-3-[(quinolin-4-ylmethyl)amino]thiophene-2-carboxamide;OSI-930 is a multi-targeted tyrosine kinase inhibitor;S1220_Selleck;OSI930;G1PEG5Q9Y2;3-[(4-Quinolinylmethyl)amino]-N-[4-(trifluoromethoxy)phenyl]-2-thiophenecarboxamide;C22H16F3N3O2S;3-((quinolin-4-ylmethyl)amino)-N-(4-(trifluoromethoxy)phenyl)thiophene-2-ca
Cas No.	728033-96-3
分子式	C₂₂H₁₆F₃N₃O₂S
分子量	443.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

OSI-930 是 Kit，KDR 和 CSF-1R (c-Fms) 的口服有效选择性抑制剂，IC₅₀ 分别为 80 nM，9 nM 和 15 nM。OSI-930 还适度抑制 Flt-1，c-Raf 和 Lck，并且对 PDGFRα/β，Flt-3 和 Abl 具有较弱的抑制活性。OSI-930 具有抗肿瘤活性。

生物活性

OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC 50 s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity.

性状

Solid

IC50 & Target[1][2]

KDR 9 nM (IC50) Flt-1 8 nM (IC50

体外研究(In Vitro)

OSI-930 inhibits cell proliferation in the HMC-1 cell line with IC50 of 14 nM but has no significant effect on the growth of COLO-205 cell line that does not express constitutively active mutant receptor tyrosine kinase.OSI-930 induces apoptosis in HMC-1 cell line with an EC50 value of 34 nM.OSI-930 inactivates purified, recombinant cytochrome P450 3A4 with a Ki of 24 μM in a time- and concentration-dependent manner has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

OSI-930 (oral gavage; once a day; 38 days; 200 mg/kg) exhibits potent antitumor activity in a broad range of preclinical xenograft models. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

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

ClinicalTrial

参考文献

[1]. Garton AJ, et al. OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Res. 2006, 66(2):1015-1024.
[2]. Lin HL, et al. Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug. Drug Metab Dispos. 2011, 39(2), 345-350.

溶解度数据	In Vitro: DMSO : 50 mg/mL (112.75 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

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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