IDH-305

• Description:

  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].

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 2

• Isoform:

  IDH1

• CAS Number:

  [1628805-46-8]