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Enasidenib

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Enasidenib is a small molecule inhibitor of the mutant isocitrate dehydrogenase 2 (IDH2) enzyme. It is designed to target the IDH2 mutation found in certain types of cancer, including acute myeloid leukemia (AML).

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Lab products found in correlation

2 hydroxypropyl β cyclodextrin, by Merck Group (2 mentions) Olaparib, by Abcam (2 mentions) D2hg assay kit, by Abcam (2 mentions) Olaparib, by Selleck Chemicals (2 mentions)

2 protocols using enasidenib

1

In vivo Olaparib and Enasidenib Pharmacokinetics

Check if the same lab product or an alternative is used in the 5 most similar protocols
Olaparib (AZD2281) (Selleckchem, Cat#S1060) was dissolved in PBS containing 10% (w/v) 2-hydroxy-propyl-beta-cyclodextrin (Sigma) at a concentration of 20mg/ml. For in vivo studies, Olaparib was administered IP at 100 mg/kg once daily. Enasidenib was purchased from LeadGen Labs, USA and dissolved in 0.5% methylcellulose and 0.2% Tween 80 in PBS at a concentration of 4 mg/ml and administered via oral gavage at 40 mg/kg once daily. 2-HG was measured in plasma before and after treatment with vehicle, Enasidenib, or Olaparib in triplicates with the D-2-Hydroxyglutarate (D2HG) assay kit (Biovision, Cat#K970–100, Sigma, Cat# MAK320–1KT) according to manufacturer’s protocol.
Gbyli R., Song Y., Liu W., Gao Y., Biancon G., Chandhok N.S., Wang X., Fu X., Patel A., Sundaram R., Tebaldi T., Mamillapalli P., Zeidan A.M., Flavell R.A., Prebet T., Bindra R.S, & Halene S. (2022). In Vivo Anti-Tumor Effect of PARP Inhibition in IDH1/2 Mutant MDS/AML Resistant to Targeted Inhibitors of Mutant IDH1/2. Leukemia, 36(5), 1313-1323.
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2

In vivo Olaparib and Enasidenib Pharmacokinetics

Check if the same lab product or an alternative is used in the 5 most similar protocols
Olaparib (AZD2281) (Selleckchem, Cat#S1060) was dissolved in PBS containing 10% (w/v) 2-hydroxy-propyl-beta-cyclodextrin (Sigma) at a concentration of 20mg/ml. For in vivo studies, Olaparib was administered IP at 100 mg/kg once daily. Enasidenib was purchased from LeadGen Labs, USA and dissolved in 0.5% methylcellulose and 0.2% Tween 80 in PBS at a concentration of 4 mg/ml and administered via oral gavage at 40 mg/kg once daily. 2-HG was measured in plasma before and after treatment with vehicle, Enasidenib, or Olaparib in triplicates with the D-2-Hydroxyglutarate (D2HG) assay kit (Biovision, Cat#K970–100, Sigma, Cat# MAK320–1KT) according to manufacturer’s protocol.
Gbyli R., Song Y., Liu W., Gao Y., Biancon G., Chandhok N.S., Wang X., Fu X., Patel A., Sundaram R., Tebaldi T., Mamillapalli P., Zeidan A.M., Flavell R.A., Prebet T., Bindra R.S, & Halene S. (2022). In Vivo Anti-Tumor Effect of PARP Inhibition in IDH1/2 Mutant MDS/AML Resistant to Targeted Inhibitors of Mutant IDH1/2. Leukemia, 36(5), 1313-1323.
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