Olutasidenib was a potent, orally available, brain-permeable, and selective mutant IDH1 (mIDH1) inhibitor with an IC50 of 21.1 nM and 114 nM for IDH1-R132H and IDH1-R132C, respectively.

 

Brand: BCM

 

Target: IDH1- R132H:21.2 nM (IC50), IDH1- R132C:114 nM (IC50)

 

In Vitro: Olutasidenib is highly selective for IDH1 isoforms, showing no appreciable inhibition against wild-type IDH1 (> 20 μM) and IDH2 mutants (R172K and R140Q: both > 20 μM). Olutasidenib effectively suppresses 2-HG production by multiple IDH1-R132 mutants (R132H, R132C, R132G, R132L), displaying Olutasidenib (FT-2102) could be efficacious against most IDH1-R132 mutant-expressing tumors.

 

Boiling Point: 603.3±55.0 °C(Predicted)

 

pKa: 10.44±0.70(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; insoluble in Ethanol.

 

Isomeric SMILES: C[C@@H](C1=CC2=C(C=CC(=C2)Cl)NC1=O)NC3=CC=C(N(C3=O)C)C#N  

 

InChIKey: NEQYWYXGTJDAKR-JTQLQIEISA-N  

 

InChI: InChI=1S/C18H15ClN4O2/c1-10(21-16-6-4-13(9-20)23(2)18(16)25)14-8-11-7-12(19)3-5-15(11)22-17(14)24/h3-8,10,21H,1-2H3,(H,22,24)/t10-/m0/s1

 

Attribute
[Chem Name]	5-[[(1S)-1-(6-chloro-2-oxo-1H-quinolin-3-yl)ethyl]amino]-1-methyl-6-oxopyridine-2-carbonitrile
[Synonym]	Olutasidenib; FT-2102; FT2102
[CAS No.]	1887014-12-1
[MDL No.]	MFCD31746915
[Formula]	C18H15ClN4O2
[Molecular]	354.79
[Form]	A crystalline solid
[Storage]	Store at -20°C

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