What Is BAY 1436032 and How Does It Work?

BAY 1436032 is a potent and selective small-molecule inhibitor targeting mutant forms of isocitrate dehydrogenase 1 (IDH1). IDH1 mutations — most commonly R132H, R132C, and related variants — are oncogenic driver mutations found in gliomas, acute myeloid leukemia (AML), cholangiocarcinoma, and other cancers. These mutations cause IDH1 to produce the oncometabolite 2-hydroxyglutarate (2-HG), which competitively inhibits α-ketoglutarate–dependent dioxygenases, leading to epigenetic dysregulation and impaired cellular differentiation.

BAY 1436032 binds to the mutant IDH1 active site, suppressing 2-HG production and thereby reversing the downstream epigenetic and differentiation blockade associated with IDH1-mutant cancers. It has demonstrated pan-IDH1 mutant inhibitory activity, covering multiple R132X variant mutations, which distinguishes it from inhibitors with narrower mutant coverage.

Solubility, Formulation, and Storage Guidelines

Proper handling of BAY 1436032 is essential to maintain compound integrity and experimental reproducibility. The following general guidelines apply; researchers should always consult the Certificate of Analysis (CoA) supplied with each lot for lot-specific data.

• Solubility: BAY 1436032 is reported to be soluble in DMSO. Prepare concentrated stock solutions in DMSO and dilute into aqueous buffers or culture media immediately before use. Minimize the final DMSO concentration in biological assays (typically ≤0.1% v/v) to avoid cytotoxicity artefacts.
• Storage: Store lyophilized powder at −20 °C, protected from light and moisture. Avoid repeated freeze-thaw cycles by preparing single-use aliquots.
• Stability: Specific stability data should be referenced from the product CoA or Selleck data sheet. As a general best practice, prepared stock solutions in DMSO should be stored at −80 °C when not in immediate use.

Note: Exact solubility values (mg/mL or mM) are not confirmed in the current source material; refer to the product CoA or contact Aladdin Scientific technical support for verified data.

Research Applications and In Vivo Use

BAY 1436032 has been investigated in multiple preclinical research contexts relevant to IDH1-mutant cancers:

• In vitro biochemical assays: Used to measure inhibition of 2-HG production in cell lysates and intact cells expressing mutant IDH1 variants.
• Cell-based differentiation studies: Applied in IDH1-mutant AML and glioma cell lines to assess restoration of normal differentiation programs upon 2-HG suppression.
• In vivo xenograft and PDX models: BAY 1436032 has demonstrated oral efficacy in preclinical mouse models, reducing tumor 2-HG levels and showing anti-tumor activity. Its oral bioavailability makes it suitable for chronic dosing regimens in rodent studies.
• Epigenetics research: Useful for studying the role of 2-HG in DNA and histone methylation, as well as TET enzyme and JMJD demethylase inhibition downstream of IDH1 mutation.

Researchers designing dose-response or mechanism-of-action studies should confirm appropriate concentrations through pilot experiments, referencing published literature for starting-point guidance.

Ordering, Quality, and Technical Support

BAY 1436032 is available from Aladdin Scientific under SKU B414041. Each order is accompanied by a Certificate of Analysis (CoA) confirming identity, purity, and lot-specific quality data. The compound corresponds to Selleck catalog number S8530, facilitating cross-referencing with published literature that cites this identifier.

For questions regarding:

• Technical specifications (purity, structural confirmation, analytical data): Contact Aladdin Scientific technical support or download the CoA from the product page.
• Custom quantities or bulk orders: Reach out to Aladdin Scientific sales representatives for quotation.
• Regulatory and safety information: Refer to the Safety Data Sheet (SDS) available on the product listing page.
• Returns and shipping: Please review Aladdin Scientific's returns, refund, and shipping policies on the website, or contact customer service.