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Catalog No.
mutant IDH1 inhibitor
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Email: [email protected]

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IC50: < 100 nM

AG-120 is an IDH1 inhibitor.

Isocitrate dehydrogenase (IDH) is a metabolic enzyme interconverting isocitrate and α-ketoglutarate (α-KG), but cancer-associated mutations of IDH1 and IDH2 confer a neomorphic activity, which allows reduction of α-KG to the oncometabolite 2-HG.

In vitro: TF-1 cells or primary human AML patient samples expressing mutant IDH1 were treated with AG-120, and the results showed that in TF-1 IDH1-R132H cells, AG-120 was able to decrease the intracellular 2-HG levels, inhibit growth factor independent proliferation and restore erythropoietin-induced differentiation [1].

Ex vivo: Previous ex-vivo study showed that the pharmacological inhibition of mutant IDH1 enzyme with AG-120 in primary human blast cells led to an effective way to lower intracellular 2-HG levels and induced myeloid differentiation [1].

Clinical trial: In a phase I clinical trial, 62 patients with advanced IDH1 mutation–positive solid tumors were treated with single agent AG-120 orally once a day. Results showed that 7 of 11 patients with IDH1 mutant–positive chondrosarcoma had stable disease; 1 out of 20 patients with IDH1 mutant–positive IHCC had a partial response and 11 patients had SD; and one out of four patients with other IDH1 mutant–positive solid tumors had SD [2].

[1] Erica Hansen et al.  AG-120, an Oral, Selective, First-in-Class, Potent Inhibitor of Mutant IDH1, Reduces Intracellular 2HG and Induces Cellular Differentiation in TF-1 R132H Cells and Primary Human IDH1 Mutant AML Patient Samples Treated Ex Vivo. Blood 2014 124:3734.
[2] http://www. ItemID=789#.WLAUOm997IU

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.1448347-49-6
Solubility≥58.3 mg/mL in DMSO; insoluble in H2O; ≥63.3 mg/mL in EtOH
Chemical Name(S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide
SDFDownload SDF
Canonical SMILESO=C([[email protected]](CC1)N(C2=NC=CC(C#N)=C2)C1=O)N([[email protected]@H](C3=CC=CC=C3Cl)C(NC4CC(F)(F)C4)=O)C5=CC(F)=CN=C5
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

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