产品
编 号：F195696
分子式：C23H22F4N6O2
分子量：490.45
分子式：C23H22F4N6O2
分子量：490.45
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1628805-46-8
产品详情
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 (IC50= 27 nM (IDH1R132H), 28 nM (IDH1R132C), 6.14 μM (IDH1WT)).
体内研究：
IDH-305 (30-300 mg/kg；口服；每天两次，持续 21 天) 抑制 IDH1 突变体 PDX 黑色素瘤模型的 2-HG 产生和 2-HG 依赖性肿瘤生长。Animal Model:nu/nu mice (HMEX2838-IDH1R132C+/-PDX model)
Dosage:30, 100, 300 mg/kg
Administration:Oral gavage; twice daily for 21 days
Result:Resulted in 62-67% 2-HG reduction and significant anti-tumor activity at 100 mg/kg and 97-99% 2-HG reduction and partial tumor regression of 32% at 300 mg/kg.
体外研究：
IDH-305 抑制 HCT116-IDH1R132H+/- 细胞，IC50 为 24 nM。
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 (IC50= 27 nM (IDH1R132H), 28 nM (IDH1R132C), 6.14 μM (IDH1WT)).
体内研究：
IDH-305 (30-300 mg/kg；口服；每天两次，持续 21 天) 抑制 IDH1 突变体 PDX 黑色素瘤模型的 2-HG 产生和 2-HG 依赖性肿瘤生长。Animal Model:nu/nu mice (HMEX2838-IDH1R132C+/-PDX model)
Dosage:30, 100, 300 mg/kg
Administration:Oral gavage; twice daily for 21 days
Result:Resulted in 62-67% 2-HG reduction and significant anti-tumor activity at 100 mg/kg and 97-99% 2-HG reduction and partial tumor regression of 32% at 300 mg/kg.
体外研究：
IDH-305 抑制 HCT116-IDH1R132H+/- 细胞，IC50 为 24 nM。
产品资料
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