Home Metabolism Dehydrogenase inhibitor BAY 1436032 For research use only.

BAY 1436032

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.

BAY 1436032 Chemical Structure

BAY 1436032 Chemical Structure

CAS: 1803274-65-8

Selleck's BAY 1436032 has been cited by 2 publications

Purity & Quality Control

Batch: S853001 DMSO] 98 mg/mL] false] Ethanol] 98 mg/mL] false] Water] Insoluble] false Purity: 99.78%
99.78

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Signaling Pathway

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Dehydrogenase Signaling Pathway

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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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models BalbC nude mice
Dosages 15-150 mg/kg
Administration by oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03127735 Completed
Leukemia Myeloid Acute
Bayer
 June 14 2017 Phase 1
NCT02746081 Active not recruiting
Solid Tumors
Bayer
 May 26 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 489.53 Formula

C26H30F3N3O3
CAS No. 1803274-65-8 SDF --
Smiles CC1CC(CC(C1)(C)C)N2C3=C(C=C(C=C3)CCC(=O)O)N=C2NC4=CC=C(C=C4)OC(F)(F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 98 mg/mL ( (200.19 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 98 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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