IDH-305

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) ) [1][2].

Product Specifications

CAS Number

[1628805-46-8]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Isocitrate Dehydrogenase (IDH)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/IDH-305.html

Concentration

10mM

Purity

99.15

Solubility

DMSO : ≥ 150 mg/mL

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

Molecular Formula

C23H22F4N6O2

Molecular Weight

490.45

Precautions

H302, H315, H319, H335

References & Citations

[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.