IDH1 Inhibitor 1
目录号: PL14797 纯度: ≥99%
CAS No. :2234285-81-3
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中文名称
IDH1 Inhibitor 1
英文名称
IDH1 Inhibitor 1
英文别名
IDH1 Inhibitor 1;BDBM50458777
Cas No.
2234285-81-3
分子式
C20H18F4N6O2
分子量
450.39
包装储存
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
产品详情
IDH1 Inhibitor 1 是一种有效的,口服生物可利用的,脑渗透性,选择性突变 IDH1 抑制剂,抑制 IDH1R132H,IDH1R132C,和 IDH1WT,IC50 分别为 0.021 μM, 0.045 μM, 和 2.52 μM。具有抗肿瘤活性。
生物活性
IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC 50 s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1, IDH1, and IDH1, respectively. Anticancer activity.
性状
Solid
IC50 & Target[1][2]
IC50: 0.021 μM (IDH1), 0.045 μM (IDH1), and 2.52 μM (IDH1)
体外研究(In Vitro)
IDH1 Inhibitor 1 (Compound 19) inhibits cellular HCT116-IDH1 with an IC50 of 0.039 μM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
IDH1 Inhibitor 1 (Compound 19) inhibits 2-hydroxyglutarate (2-HG) production in a preclinical xenograft tumor model. IDH1 Inhibitor 1 is also profiled in a patient-derived IDH1 mutant HCT116-IDH1 mechanistic xenograft tumor model in mice to evaluate in vivo inhibition of 2-HG production. IDH1 Inhibitor 1, dosed orally at 150 mg/kg, inhibits new 2-HG production. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Zhao Q, et al. Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors. ACS Med Chem Lett. 2018 Jun 11;9(7):746-751.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (222.03 mM)配制储备液
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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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