BAY 1436032

Catalog No.S8530

BAY 1436032 Chemical Structure

Molecular Weight(MW): 489.53

BAY-1436032 is a highly selective, potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). 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.

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Biological Activity

Description BAY-1436032 is a highly selective, potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). 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.
Targets
IDH1 (R132H) [1]
(Cell-free assay)
IDH1 (R132C) [1]
(Cell-free assay)
15 nM 15 nM
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[1].

In vivo

The pharmacokinetic properties of BAY 1436032 allow for oral administration. In vivo pharmacokinetics (PK) in rats shows low CL and high oral bioavailability. Oral administration of BAY 1436032 confers a survival benefit to mice transplanted with IDH1 mutant tumors. BAY 1436032 induces differentiation in intracranial xenografts[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: NCH551b patient-derived glioma cell lines
  • Concentrations: 500 nM and 2.5 µM
  • Incubation Time: 1 day
  • Method:

    Cells are seeded with 4000 cells/well in 96-well plates for suspension cells. For each condition, three wells are used. The cells are treated 1 day after seeding with BAY 1436032 at concentrations of 500 nM and 2.5 µM and DMSO as solvent control. Subsequently, measurements are performed on days 7, 14 and 21 after the first inhibitor treatment. The cells receive fresh drug-containing medium after the first 7 and 14 days of treatment. Plates are measured with a microplate reader.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: BalbC nude mice
  • Formulation: --
  • Dosages: 15-150 mg/kg
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 98 mg/mL (200.19 mM)
Ethanol 98 mg/mL (200.19 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 489.53
Formula

C26H30F3N3O3

CAS No. 1803274-65-8
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID