IDH1 Inhibitor 1


CAS No. : 2234285-81-3

2234285-81-3
Price and Availability of CAS No. : 2234285-81-3
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5mg $780 In-stock
10mg $1250 In-stock
25mg $2580 In-stock
50mg $3500 In-stock
100mg $4780 In-stock
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Cat. No. : HY-112601
M.Wt: 450.39
Formula: C20H18F4N6O2
Purity: >98 %
Solubility: DMSO : ≥ 100 mg/mL
Introduction of 2234285-81-3 :

IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively[1]. Anticancer activity[1]. IC50 & Target: IC50: 0.021 μM (IDH1R132H), 0.045 μM (IDH1R132C), and 2.52 μM (IDH1WT)[1] In Vitro: IDH1 Inhibitor 1 (Compound 19) inhibits cellular HCT116-IDH1R132H/+ with an IC50 of 0.039 μM[1]. In Vivo: IDH1 Inhibitor 1 (Compound 19) inhibits 2-hydroxyglutarate (2-HG) production in a preclinical xenograft tumor model. IDH1 Inhibitor 1 is also profiled in a patient-derived IDH1 mutant HCT116-IDH1R132H/+ mechanistic xenograft tumor model in mice to evaluate in vivo inhibition of 2-HG production. IDH1 Inhibitor 1, dosed orally at 150 mg/kg, inhibits new 2-HG production[1].

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