[CAS NO. 1803274-65-8] BAY 1436032
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PRODUCTS SPECIFICATIONS [1803274-65-8]
Distributor
Catalog
AS941201
Brand
Arctom Scientific
CAS
1803274-65-8
DESCRIPTION [1803274-65-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 489.53 |
| Molecular Formula | C26H30F3N3O3 |
| SMILES | O=C(O)CCC1=CC=C2N([C@H]3CC(C)(C)C[C@@H](C)C3)C(NC4=CC=C(OC(F)(F)F)C=C4)=NC2=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0428 mL | 10.2139 mL | 20.4278 mL |
| 5 mM | 0.4086 mL | 2.0428 mL | 4.0856 mL |
| 10 mM | 0.2043 mL | 1.0214 mL | 2.0428 mL |
| 50 mM | 0.0409 mL | 0.2043 mL | 0.4086 mL |
Description
BAY-1436032 is a highly selective, potent and orally available inhibitor of . It is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displays potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants.
In vitro
BAY 1436032 exhibits an IC50 of 15 nM for mutant IDH1R132H protein and virtually no effect on wild-type IDH1 and the structurally related IDH2 proteins with IC50 of 20 and >100 µM, respectively. BAY 1436032 not only reduces 2-HG levels in cells with the IDH1R132H or the IDH1R132C mutations, but also in those with the R132G, R132S or R132L mutations with equal efficiency. There is no inhibition of IDH2 R172M. BAY 1436032 reduces proliferation and induces differentiation in primary glioma cultures. BAY 1436032 reveals low metabolic clearance (CL) in vitro in rat hepatocytes and mice liver microsomes.
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