Mutant IDH1-IN-1|DC Chemicals

Cas No.:	1355326-21-4
SMILES:	CC1=CC=CC=C1C(N(C(CN2C=NC3=CC=CC=C32)=O)C4=CC=CC(F)=C4)/C(O)=N/C5CCCCC5
Formula:	C₃₀H₃₁FN₄O₂
M.Wt:	498.59
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.
Target:	IC50: 4 nM (IDH1 R132C/R132C), 42 nM (IDH1 R132H/R132H), 80 nM (IDH1 R132H/WT), 143 nM (IDH1 wild type)[1]
References:	[1]. Deng G, et al. Selective inhibition of mutant isocitrate dehydrogenase 1 (IDH1) via disruption of a metal binding network by an allosteric small molecule. J Biol Chem. 2015 Jan 9;290(2):762-74.

Cat. No.	Product name	Field of application
DC7982	Mutant IDH1-IN-1	Mutant IDH1-IN-1 is a potent mutant IDH1 R132H inhibitor with IC50 < 0.1 uM(A level in Patent).
DC10830	IDH-889	IDH889 is a potent and selective inhibitors of IDH1. IDH899 shows IDH (R132H) IC50 = 20 nM; Cell 2-HG IC50 = 14 nM.
DC10538	IDH-305	IDH305 is an inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity.
DC7174	AGI-6780	AGI-6780 is the first highly potent and selective small molecule inhibitor of isocitrate dehydrogenases, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q (IC50=23 nM).
DC5050	AGI-5198	AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.
DC10439	Vorasidenib (AG881)	AG-881 is a potent and selective orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1) in the cytoplasm and type 2 (IDH2).
DC8374	Enasidenib ( AG-221)	Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively.
DC8051	AG-120 (Ivosidenib)	AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein.