IDH305( IDH-305 | IDH 305 )

Catalog No. M12434 CAS No. 1628805-46-8

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

IDH305
Note

Research use only, not for human use.
Brief Description

IDH 305 (IDH305) is a potent, selective, brain penetrant mutant IDH1 inhibitor with IC50 of 18 and 28 nM for IDH1 R132H and R132C.
Description

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.
In Vitro

——
In Vivo

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.
Synonyms

IDH-305 | IDH 305
Pathway

Metabolic Enzyme/Protease
Target

IDH
Recptor

IDH
Research Area

Cancer
Indication

Brain Cancer

CAS Number

1628805-46-8
Formula Weight

490.463
Molecular Formula

C23H22F4N6O2
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 150 mg/mL 305.84 mM
SMILES

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
Chemical Name

(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

1. Cho YS, et al. ACS Med Chem Lett. 2017 Sep 18;8(10):1116-1121.

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