Ivosidenib

SKU: orb1226253

Description

A mutant-selective inhibitor of IDH1 (isocitrate dehydrogenase type 1); represent a worthwhile avenue of exploration in the treatment of IDH1-mutated tumors.Blood Cancer Phase 3 Clinical(In Vitro):Ivosidenib (AG-120) (0-13 μM; 48 hours) inhibits several IDH1-R132 mutants with potency similar IC50 values: IDH1-R132H (IC50=12 nM); IDH1-R132C (IC50=13 nM); IDH1-R132G (IC50=8 nM); IDH1-R132L (IC50=13 nM); IDH1-R132S (IC50=12 nM), respectively.(In Vivo):AG-120 (gavage administration; 50 mg/kg and 150 mg/kg) declines tumor 2-HG concentration rapidly, with maximum inhibition (92.0% and 95.2% at the 50 mg/kg and 150 mg/kg doses, respectively) achieved at -12 h post dose.

Key Properties

• CAS Number: 1448347-49-6
• MW: 582.9609
• Purity: >98% (HPLC)
• Formula: C₂₈H₂₂ClF₃N₆O₃
• SMILES: C1CC(=O)N(C1C(=O)N(C2=CC(=CN=C2)F)C(C3=CC=CC=C3Cl)C(=O)NC4CC(C4)(F)F)C5=NC=CC(=C5)C#N
• Target: IDH
• Solubility: DMSO: ≥ 39 mg/mL

Bioactivity

• In Vivo:
  AG-120 (gavage administration; 50 mg/kg and 150 mg/kg) declines tumor 2-HG concentration rapidly, with maximum inhibition (92.0% and 95.2% at the 50 mg/kg and 150 mg/kg doses, respectively) achieved at-12 h post dose. Animal model: Female nude BALB/c mice inoculated with HT1080 cells. Dosage: 50 mg/kg and 150 mg/kg. Administration: Gavage administration; 50 mg/kg and 150 mg/kg. Result: Showed robust tumor 2-HG reduction in mouse.
• In Vitro:
  Ivosidenib (AG-120) (0-13 μM; 48 hours) inhibits several IDH1-R132 mutants with potency similar IC50 values: IDH1-R132H (IC50 = 12 nM); IDH1-R132C (IC50 = 13 nM); IDH1-R132G (IC50 = 8 nM); IDH1-R132 L (IC50 = 13 nM); IDH1-R132S (IC50 = 12 nM), respectively.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AG-120

Quick Database Links

Gene Symbol

IDH