1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)
  3. Ivosidenib

Ivosidenib (Synonyms: AG-120)

Cat. No.: HY-18767 Purity: 99.24% ee.: 99.51%
Handling Instructions

Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity.

For research use only. We do not sell to patients.

Ivosidenib Chemical Structure

Ivosidenib Chemical Structure

CAS No. : 1448347-49-6

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10 mM * 1 mL in DMSO USD 123 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Ivosidenib:

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  • Biological Activity

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Description

Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity[1].

IC50 & Target

12 nM (mouse IDH1R132H)[1]

In Vitro

Ivosidenib (AG-120) (0-13 μM; 48 hours) inhibits several IDH1-R132 mutants with potency similar IC50 values: IDH1-R132H (IC50=12 μM); IDH1-R132C (IC50=13 μM); IDH1-R132G (IC50=8 μM); IDH1-R132L (IC50=13 μM); IDH1-R132S (IC50=12 μM), respectively[1].

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[1].

Animal Model: Female nude BALB/c mice inoculated with HT1080 cells[1]
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.
Clinical Trial
Molecular Weight

582.96

Formula

C₂₈H₂₂ClF₃N₆O₃

CAS No.

1448347-49-6

SMILES

ClC1=C([[email protected]](N(C2=CC(F)=CN=C2)C([[email protected]]3N(C4=NC=CC(C#N)=C4)C(CC3)=O)=O)C(NC5CC(F)(F)C5)=O)C=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 39 mg/mL (66.90 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7154 mL 8.5769 mL 17.1538 mL
5 mM 0.3431 mL 1.7154 mL 3.4308 mL
10 mM 0.1715 mL 0.8577 mL 1.7154 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.24% ee.: 99.51%

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KeyWords:

Ivosidenib | AG-120 | AG120 | AG 120 | Isocitrate Dehydrogenase (IDH) | Inhibitor | inhibitor | inhibit

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