Enasidenib ag 221

Manufactured by MedChemExpress

Sourced in United States

Enasidenib (AG-221) is a small molecule inhibitor that selectively targets the mutant isocitrate dehydrogenase 2 (IDH2) enzyme. IDH2 mutations are frequently found in various hematological malignancies, including acute myeloid leukemia (AML).

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Lab products found in correlation

Dimethyl α ketoglutarate dmkg, by Merck Group (1 mentions) Enasidenib, by Merck Group (1 mentions) Tween 80, by Merck Group (1 mentions) Methylcellulose, by Merck Group (1 mentions) Metformin, by Selleck Chemicals (1 mentions) Ivosidenib, by Selleck Chemicals (1 mentions) Cb 839, by Selleck Chemicals (1 mentions) Bay 1436032, by MedChemExpress (1 mentions) Agi 6780, by MedChemExpress (1 mentions) Gsk864, by Merck Group (1 mentions)

Spelling variants of this product

AG-221 (2 citations) Enasidenib (2 citations)

3 protocols using enasidenib ag 221

Comparative Analysis of Bioactive Beta-Glucans

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Paramylon (CAS: 9051-97-2), a linear β- (1,3)-D-glucan without any branches, has a molecular weight of about 500,000 Da and is insoluble. Laminarin (CAS: 9008-22-4), a β- (1,3)-D-glucan containing several β- (1,6) interchain junctions and branch points, has a molecular weight up to 500Da and is soluble. Both commercial β-Glucans mentioned above were purchased from Sigma-Aldrich (USA). Enasidenib (AG-221; CAS: 1446502-11-9; Purity 99.97%) was purchased from Med Chem Express (USA). Dimethyl-α-Ketoglutarate (DMKG; CAS: 13192-04-6; Purity ≥ 95.5%) was purchased from Sigma-Aldrich (USA). Prior to use, β-glucans were dissolved in sterile PBS to a final concentration of 1 mg/mL, and insoluble Paramylon was mixed by repeated blowing with a pipettor.

Wu Z., Yang Y., Li J., Bossier P., Wei X., Guo Z., Han B, & Ye J. (2023). β-Glucans in particulate and solubilized forms elicit varied immunomodulatory and apoptosis effects in teleost macrophages in a dosedependent manner. Frontiers in Immunology, 14, 1243358.

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Preparation of Small Molecule Inhibitors

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enasidenib (AG-221) was purchased from MedChemExpress (Cat#HY-18690, Monmouth Junction, NJ, USA) and ivosidenib (AG-120), vorasidenib (AG-881), AGI-5198, DS-1001b, metformin and CB-839 were acquired from Selleckchem (Cat#S8206, #S8611, #S7185, #S8881, #S1950 and #S7655, respectively, Houston, TX, USA). Stocks for in vitro experiments were prepared as 10 mM solutions in sterile DMSO, stored at −80 °C and diluted in culture medium to the final concentration just before use. For in vivo treatments, enasidenib was solubilized in distilled water containing 0.5% methylcellulose (Cat#M7027, Sigma–Aldrich, St Louis, MO, USA) and 0.2% Tween-80 (Cat#P8074, Sigma–Aldrich) before administration.

Rey V., Tornín J., Alba-Linares J.J., Robledo C., Murillo D., Rodríguez A., Gallego B., Huergo C., Viera C., Braña A., Astudillo A., Heymann D., Szuhai K., Bovée J.V., Fernández A.F., Fraga M.F., Alonso J, & Rodríguez R. (2024). A personalized medicine approach identifies enasidenib as an efficient treatment for IDH2 mutant chondrosarcoma. eBioMedicine, 102, 105090.

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Detailed Compound Characterization Protocol

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Chemicals were used as purchased
and were >95% pure by HPLC according to the commercial suppliers.
Ivosidenib (AG-120), AGI-5198, Agios 135 (HY-12475), Novartis 224
(HY-18717), Novartis 556 (HY-13972), Vorasidenib (AG-881), BAY-1436032,
AGI-6780, and Enasidenib (AG-221) were purchased from MedChem Express.
ML309 hydrochloride, GSK864, and Sanofi 1 (SML1430) were purchased
from Sigma-Aldrich. SYC-435 (TC-E 5008) was purchased from Bio-Techne.

Liu S., Abboud M., Mikhailov V., Liu X., Reinbold R, & Schofield C.J. (2023). Differentiating Inhibition Selectivity and Binding Affinity of Isocitrate Dehydrogenase 1 Variant Inhibitors. Journal of Medicinal Chemistry, 66(7), 5279-5288.

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