IDH-305

SKU: orb1308209

Description

IDH-305 is a brain-penetrant, orally bioavailable small molecule inhibitor with high selectivity for mutant IDH1 (R132H/C) over the wild-type enzyme. It is a research tool for investigating mutant IDH1-driven pathologies, such as glioma and cholangiocarcinoma, in both cellular and animal models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1628805-46-8
• MW: 490.45
• Purity: 99.68% (May vary between batches)
• Formula: C₂₃H₂₂F₄N₆O₂
• SMILES: C[C@H](F)[C@H]1COC(=O)N1c1ccnc(N[C@@H](C)c2cc(C)c(cn2)-c2ccnc(c2)C(F)(F)F)n1
• Target: Dehydrogenase,Isocitrate Dehydrogenase (IDH)
• Solubility: DMSO:100 mg/mL (203.89 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.16 mM)

Bioactivity

• Target IC50:
  IDH1 (WT):6.14 μM|IDH1 (R132H):27 nM|IDH1 (R132C):28 nM
• In Vivo:
  P.o. administration of 30-300 mg/kg IDH-305 twice daily for 21 days suppresses 2-HG production and 2-HG-dependent tumor growth of an IDH1 mutant PDX melanoma model .
• In Vitro:
  IDH-305 suppresses HCT116-IDH1R132H /- cells (IC50 of 24 nM).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Isocitrate Dehydrogenase (IDH), IDH1WT, IDH1R132C, IDH 305, IDH1-R132C, IDH1R132H, IDH1-R132H, IDH1-WT, IDH305, IDH-305, Inhibitor

Compound Identifiers

PubChem CID

90415637