| Identification | Back Directory | [Name]
1H-Pyrazolo[4,3-c]pyridine-3-carboxamide, 1-[(4-fluorophenyl)methyl]-4,5,6,7-tetrahydro-N-[3-[(1R)-1-hydroxyethyl]phenyl]-7-methyl-5-(1H-pyrrol-2-ylcarbonyl)-, (7S)- | [CAS]
1816272-18-0 | [Synonyms]
(S,R)-GSK321
(S,R)-WT IDH1 Inhibitor 2
1H-Pyrazolo[4,3-c]pyridine-3-carboxamide, 1-[(4-fluorophenyl)methyl]-4,5,6,7-tetrahydro-N-[3-[(1R)-1-hydroxyethyl]phenyl]-7-methyl-5-(1H-pyrrol-2-ylcarbonyl)-, (7S)- | [Molecular Formula]
C28H28FN5O3 | [MOL File]
1816272-18-0.mol | [Molecular Weight]
501.55 |
| Chemical Properties | Back Directory | [Boiling point ]
704.2±60.0 °C(Predicted) | [density ]
1.35±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
12.26±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
(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]. | [IC 50]
IDH1 | [References]
[1] Okoye-Okafor UC, et, al. New IDH1 mutant inhibitors for treatment of acute myeloid leukemia. Nat Chem Biol. 2015 Nov;11(11):878-86. DOI:10.1038/nchembio.1930 |
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