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Ivosidenib

Cat. No. M8958
Ivosidenib Structure
Synonym:

AG-120

Size Price Availability Quantity
5mg USD 120 In stock
25mg USD 400 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Ivosidenib is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Ivosidenib specifically inhibits a mutated form of IDH1 in the cytoplasm, which inhibits the formation of the oncometabolite, 2-hydroxyglutarate (2HG).

In vitro, TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with AG-120.Treatment with AG-120 decreases intracellular 2-HG levels, inhibites growth factor independent proliferation and restores erythropoietin (EPO)-induced differentiation in TF-1 IDH1-R132H cells.

Protocol
Cell Experiment
Cell lines TF-1 cells
Preparation method TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with AG-120.
Concentrations 0.5, 1.0, and 5.0 μM
Incubation time 6 days
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 582.96
Formula C28H22ClF3N6O3
CAS Number 1448347-49-6
Purity >99%
Solubility DMSO: ≥ 60 mg/mL
Storage at -20°C
References

Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers.
Popovici-Muller J, et al. ACS Med Chem Lett. 2018 Jan 19;9(4):300-305. PMID: 29670690.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Ivosidenib, AG-120 supplier, Dehydrogenase, inhibitors

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