1816272-18-0
Chemical Structure
(S,R)-GSK321
- CAS No.: 1816272-18-0
- Formula:C28H28FN5O3
- Molecular Weight:501.55
IUPAC Name: (S)-1-(4-fluorobenzyl)-N-(3-((R)-1-hydroxyethyl)phenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-3-carboxamide
InChIKey: IVFDDVKCCBDPQZ-ZWKOTPCHSA-N
SMILES: C[C@@H](O)C1=CC=CC(NC(C2=NN(C3=C2CN(C[C@@H]3C)C(C4=CC=CN4)=O)CC5=CC=C(C=C5)F)=O)=C1
Biological Activity: (S,R)-GSK321 is the (S,R)-enantiomer of GSK321 (HY-18948). GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. GSK321 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. GSK321can be used for research of acute myeloid leukemia (AML) and other cancers[1].
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(S,R)-GSK321 | 98.62% | (S,R)-GSK321 is the (S,R)-enantiomer of GSK321 (HY-18948). GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. GSK321 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. GSK321can be used for research of acute myeloid leukemia (AML) and other cancers. | ||||||||||||||||||||
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