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BAY-1436032

Chemical Structure : BAY-1436032

CAS No.: 1803274-65-8

BAY-1436032 (BAY1436032;BAY 1436032)

Catalog No.: PC-60292Not For Human Use, Lab Use Only.

BAY-1436032 (BAY1436032) is a potent, selective, orally available inhibitor of pan-mutant IDH1 with IC50 of 15 nM for both IDH1 R132H and R132C, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BAY-1436032 (BAY1436032) is a potent, selective, orally available inhibitor of pan-mutant IDH1 with IC50 of 15 nM for both IDH1 R132H and R132C, respectively; shows no effect on wild-type IDH1; strongly reduces 2-HG levels in cells carrying IDH1-R132H, -R132C, -R132G, -R132S and -R132L mutations; significantly prolongs survival of mice intracerebrally transplanted with human astrocytoma carrying the IDH1R132H mutation.

Blood Cancer

Phase 1 Clinical

Physicochemical Properties

M.Wt 489.54
Formula C26H30F3N3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(2-((4-(trifluoromethoxy)phenyl)amino)-1-((1R,5R)-3,3,5-trimethylcyclohexyl)-1H-benzo[d]imidazol-5-yl)propanoic acid

References

1. Pusch S, et al. Acta Neuropathol. 2017 Apr;133(4):629-644.

2. Chaturvedi A, et al. Leukemia. 2017 Oct;31(10):2020-2028.

3. Gokul S, et al. CNS Neurol Disord Drug Targets. 2017;16(6):636-637.

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