IDH-305|1628805-46-8|-陌孚医药/Medlife

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IDH-305

目录号: PL14806 纯度: ≥98%

CAS No. :1628805-46-8

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中文名称	IDH-305
中文别名	IDH抑制剂(IDH-305);(R)-4-((S)-1-氟乙基)-3-(2-(((S-1-(4-甲基-2'-(三氟甲基)-[3,4'-联吡啶]-6-基)乙基)氨基)嘧啶-4-基)恶唑烷-2-酮;化合物IDH-305
英文名称	IDH-305
英文别名	IDH-305;A791KH7YZW;(4R)-4-[(1S)-1-fluoroethyl]-3-[2-[[(1S)-1-[4-methyl-5-[2-(trifluoromethyl)pyridin-4-yl]pyridin-2-yl]ethyl]amino]pyrimidin-4-yl]-1,3-oxazolidin-2-one;(4R)-4-[(1S)-1-fluoroethyl]-3-(2-{[(1S)-1-[4-methyl-2'-(trifluoromethyl)-[3,4'-bipyridin]-6-yl]ethyl]amino}pyrimidin-4-yl)-1,3-oxazolidin-2-one;(4R)-4-[(1S)-1-fluoroethyl]-3-[2-({(1S)-1-[4-methyl-2'-(trifluoromethyl)[3,4'-bipyridin]-6-yl]ethyl}amino)pyrimidin-4-yl]-1,3-oxazolidin-2-one;IDH305;IDH 305;2-Oxazolidinone, 4-[(1S)-1-fluoroethyl]-3-[2-[[(1S)-1-[4-methyl-2'-(trifluoromethyl)[3,4'-bipyridin]-6-yl]ethyl]amino]-4-pyrimidinyl]-, (4R)-;(4R)-4-[(1S)-1-Fluoroethyl]-3-[2-[[(1S)-1-[4-methyl-2'-(trifluoromethyl)[3,4'-bipyridin]-6-yl]ethyl]amino]-4-pyrimidinyl]-2-oxazolidinone
Cas No.	1628805-46-8
分子式	C₂₃H₂₂F₄N₆O₂
分子量	490.45
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

IDH-305 是一种口服性、突变选择性和脑渗透性的 IDH1 抑制剂，靶向 IDH1 (R132) 突变。IDH-305 对突变体 IDH1 亚型的选择性比野生型高 200 倍 (IC₅₀= 27 nM (IDH1^R132H), 28 nM (IDH1^R132C), 6.14 µM (IDH1^WT))。

生物活性

IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC 50 = 27 nM (IDH1), 28 nM (IDH1), 6.14 μM (IDH1)).

性状

Solid

IC50 & Target[1][2]

IC50: 27 nM (IDH1), 28 nM (IDH1), 6.14 μM (IDH1)

体外研究(In Vitro)

IDH-305 inhibits HCT116-IDH1 cells with an IC50 of 24 nM. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

IDH-305 (30-300 mg/kg; p.o.; twice daily for 21 days) inhibits 2-HG production and 2-HG-dependent tumor growth of an IDH1 mutant PDX melanoma model. 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]. Cho YS, et al. Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor. ACS Med Chem Lett. 2017 Sep 18;8(10):1116-1121.
[2]. Courtney D DiNardo, et al. A Phase I Study of IDH305 in Patients with Advanced Malignancies Including Relapsed/Refractory AML and MDS That Harbor IDH1R132 Mutations. Blood, 128(22), 1073.

溶解度数据	In Vitro: DMSO : ≥ 150 mg/mL (305.84 mM)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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