IDH305

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

IDH 305 (IDH305) 是一种有效的、选择性的、脑渗透性突变 IDH1 抑制剂，对 IDH1 R132H 和 R132C 的 IC50 分别为 18 和 28 nM。

IDH 305 (IDH305)?is a potent, selective, brain penetrant mutant IDH1 inhibitor with IC50 of 18 and 28 nM for IDH1 R132H and R132C; exhibits >200 fold selectivity over WT IDH1 (IC50=6.14 uM), and no activtiy against IDH2 mutants; inhibits EGF-independent proliferation of HCT116-IDH1R132H+/- cells with IC50 of 20 nM; exhibits in vivo correlation of 2-HG reduction and efficacy in IDH1 mutant xenograft tumor model.Brain Cancer Phase 1 Clinical.

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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.

IDH-305 | IDH 305

Metabolic Enzyme/Protease

IDH

IDH

Cancer

Brain Cancer

1628805-46-8

490.463

C23H22F4N6O2

>98% (HPLC)

DMSO : ≥ 150 mg/mL 305.84 mM

O=C1OC[C@H]([C@@H](F)C)N1C2=NC(N[C@H](C3=CC(C)=C(C4=CC(C(F)(F)F)=NC=C4)C=N3)C)=NC=C2

(R)-4-((S)-1-fluoroethyl)-3-(2-(((S)-1-(4-methyl-2'-(trifluoromethyl)-[3,4'-bipyridin]-6-yl)ethyl)amino)pyrimidin-4-yl)oxazolidin-2-one

(-20℃)

With Ice Pack

≥ 2 years