An inhibitor of mutant IDH1 (IC50s = 15 and 130 nM for IDH1R132H and IDH1R132C

DS-1001b – 5 mg

Brand:
Cayman
CAS:
1898207-64-1
Storage:
-20
UN-No:
Non-Hazardous - /

DS-1001b is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 15 and 130 nM for IDH1R132H and IDH1R132C, respectively).{60060} It is selective for mutant IDH1, which converts α-ketoglutarate to the oncometabolite 2-hydroxyglutarate (2-HG), over wild-type IDH1 and IDH2, which convert isocitrate to α-ketoglutarate, as well as IDH2R140Q and IDH2R172Q (IC50s = >10,000 nM for all). DS-1001b inhibits 2-HG production in TF-1 cells stably transfected with IDH1R132H or IDH1R132C (IC50s = 29 and 35 nM, respectively) and in 293A cells transiently transfected with IDH1R132H or IDH1R132C (IC50s = 29 and 42 nM, respectively). DS-1001b reduces tumor growth, as well as intratumoral and plasma 2-HG levels, in a subcutaneous IDH1R132H-expressing A1074 patient-derived xenograft (PDX) mouse model of glioblastoma.  

 

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SKU: 31488 - 5 mg Category:

Description

An inhibitor of mutant IDH1 (IC50s = 15 and 130 nM for IDH1R132H and IDH1R132C, respectively); selective for mutant IDH1 over wild-type IDH1 and IDH2, as well as IDH2R140Q and IDH2R172Q (IC50s = >10,000 nM for all); inhibits 2-HG production in TF-1 cells stably transfected with IDH1R132H or IDH1R132C (IC50s = 29 and 35 nM, respectively) and in 293A cells transiently transfected with IDH1R132H or IDH1R132C (IC50s = 29 and 42 nM, respectively); reduces tumor growth, as well as intratumoral and plasma 2-HG levels, in a subcutaneous IDH1R132H-expressing A1074 PDX mouse model of glioblastoma

Formal name: (2E)-3-[1-[[5-(1-fluoro-1-methylethyl)-3-(2,4,6-trichlorophenyl)-4-isoxazolyl]carbonyl]-3-methyl-1H-indol-4-yl]-2-propenoic acid, compd. with 2-methyl-2-propanamine (1:1)

Synonyms: 

Molecular weight: 608.9

CAS: 1898207-64-1

Purity: ≥98%

Formulation: A crystalline solid

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