BAY-1436032

SKU: orb1296249

Description

BAY-1436032 is a potent, orally bioavailable small molecule inhibitor that selectively targets pan-mutant IDH1 enzymes. It is utilized in preclinical research to investigate mutant IDH1-driven mechanisms in cancers such as glioma, with studies demonstrating its activity in both cellular assays and in vivo models.

Research Area

Metabolism Research

Images & Validation

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Key Properties

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CAS Number	1803274-65-8
MW	489.53
Purity	99.38% (May vary between batches)
Formula	C₂₆H₃₀F₃N₃O₃
SMILES	C[C@H]1C[C@H](CC(C)(C)C1)n1c(Nc2ccc(OC(F)(F)F)cc2)nc2cc(CCC(O)=O)ccc12
Target	Isocitrate Dehydrogenase (IDH),Dehydrogenase
Solubility	DMSO:120 mg/mL (245.13 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.17 mM)

Bioactivity

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In Vivo	Long-term exposure to once-daily oral BAY-1436032 reveals nearly complete suppression of R-2HG production with 150 mg/kg BAY1436032. White blood cell counts constantly increase in vehicle-treated mice and, at a lower rate, in animals receiving 45 mg/kg BAY-1436032, while they remain constant in the 150 mg/kg cohort. Hemoglobin levels are slightly lower in the vehicle and 45 mg/kg groups as compared to the 150 mg/kg cohort at day 60, while platelet counts are significantly reduced in the vehicle and 45 mg/kg BAY-1436032 treated mice compared to the 150 mg/kg cohort at day 60. All mice receiving 150 mg/kg BAY-1436032 survive with minimal hCD45+ cell load in their peripheral blood until the end of observation at day 150 after treatment start, while vehicle-treated animals die from leukemia with a median survival of 91 days. Mice treated with 45 mg/kg BAY-1436032 display intermediate levels of CD14/CD15 expression. Read more...
In Vitro	BAY-1436032 inhibits intracellular (R)-2-hydroxyglutarate (R-2HG) production in mouse hematopoietic cells expressing IDH1R132H or IDH1R132C (IC50s: 60 and 45 nM). R-2HG levels are not reduced in IDH2R140Q and IDH2R172K expressing mouse hematopoietic cells by BAY-1436032 at concentrations up to 10 μM. Colony growth is inhibited by 50% at a concentration of 0.1 μM BAY-1436032, while concentrations up to 100 μM do not suppress colony growth of patient-derived IDH1 wild-type AML cells. On morphologic evaluation myelomonocytic differentiation of myeloid progenitors is strongly induced by BAY-1436032. Read more...
Cell Research	Colony-forming cell (CFC) units are assayed in methylcellulose supplemented with 10 ng/mL IL-3, 10 ng/mL GM-CSF, 50 ng/ mL SCF, 50 ng/mL FLT3-ligand and 3 U/mL EPO. Vehicle or BAY-1436032 is added to methylcellulose containing 1 × 10^5 human mononuclear cells, which are plated in duplicate. Colonies are evaluated microscopically 10 to 14 days after plating by standard criteria. Read more...
Animal Research	NSG mice are used and transplanted with primary acute myeloid leukemia (AML) cells from a patient with IDH1R132C mutant AML. Per condition 10 mice are treated with vehicle, 45 or 150 mg/kg body weight BAY-1436032 once daily by oral gavage for 150 days starting 17 days after transplantation. Finally, serum R-2HG levels and human CD45+ (hCD45+) cells are measured. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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BAY1436032, BAY-1436032, BAY 1436032, inhibit, Isocitrate Dehydrogenase (IDH), IsocitrateDehydrogenase, IsocitrateDehydrogenase(IDH), Isocitrate Dehydrogenase, IDH, IDH1, Inhibitor

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Compound Identifiers

PubChem CID

118310260 ↗

Key Properties

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No computed properties available.

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Purity:	>98% (HPLC)
CAS Number:	1803274-65-8
MW:	489.54
Formula:	C₂₆H₃₀F₃N₃O₃

BAY-1436032

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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