Ivosidenib

Ivosidenib represents a targeted therapeutic approach for the treatment of acute myeloid leukemia with IDH1 mutations. As a first-in-class mIDH1 inhibitor, Ivosidenib specifically targets the mutated form of IDH1 in the cytoplasm, inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG). Ivosidenib inhibits several IDH1-R132 mutants with potent IC₅₀ values: IDH1-R132H (12 nM), IDH1-R132G (13 nM), IDH1-R132L (13 nM), and IDH1-R132S (12 nM). In vivo, Ivosidenib demonstrates rapid and profound tumor 2-HG concentration reduction, with maximum inhibition of 92.0-95.2% achieved at 12 hours post-dose. Ivosidenib has the potential for AML therapy due to its acceptable safety profile and clinical activity. By inhibiting 2-HG production, Ivosidenib induces cellular differentiation and inhibits proliferation in IDH1-expressing tumor cells.

 

Product Parameters

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Parameter	Specification
Product Name	Ivosidenib
CAS Number	1448347-49-6
Molecular Formula	C₂₈H₂₂ClF₃N₆O₃
Molecular Weight	582.96 g/mol
Appearance	White to off-white solid
Melting Point	151-173 °C
Boiling Point	854.3±65.0 °C
Storage (Powder)	-20°C Freezer, Under inert atmosphere

 

Small Molecule Inhibitors

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Tibsovo (brand name: Alevonib) is an oral, targeted small-molecule inhibitor of isocitrate dehydrogenase-1 (IDH1), and the first approved potent oral targeted inhibitor in China for cancers with IDH1 mutations. Initially developed by Agios Pharmaceuticals, the drug was subsequently developed and commercialized by CStone Pharmaceuticals in Greater China and expanded to Singapore. Tibsovo is indicated for the treatment of adult patients with relapsed or refractory acute myeloid leukemia (R/RAML) harboring IDH1 susceptibility mutations. The recommended dosage is 500 mg daily orally until disease progression or development of intolerable toxicity. Tibsovo has been approved by the FDA in the United States for multiple indications, including AML and cholangiocarcinoma. However, Tibsovo may cause a range of adverse effects, such as gastrointestinal disturbances, hepatic dysfunction, and anemia; therefore, close monitoring of patient response is essential during administration.

 

Bioactivity

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Ivosidenib (AG-120) is an orally active IDH1 (isocitrate dehydrogenase type 1) inhibitor with potential antitumor activity.

 

In Vitro Study

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Treatment of TF-1 cells and primary human AML patient samples harboring the IDH1 mutation with AG-120 reduced intracellular 2-HG levels, inhibited growth factor-independent cell proliferation, and restored erythropoietin-induced cell differentiation in TF-1 ChemicalbookIDH1-R132H cells. Similarly, inhibition of the mutated IDH1 by AG-120 in primary human progenitor cells effectively decreased 2-HG levels and induced myeloid differentiation.

 

Contact Us

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Looking for Ivosidenib for your oncology research, IDH1 inhibitor development, or targeted therapy program? Cosperpharm is your trusted partner for high-purity research compounds. Reach out today — let's discuss how we can support your project with quality material and expert service.