BAY-1436032 free base · Synonyms: BAY 1436032 · BAY1436032

BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 inhibitor.

For research use only. Not for human or veterinary use.

Target Isocitrate Dehydrogenase (IDH)

Research area Cancerv

Purity >98% Stock Inquire

Data Sheet SDS COA

BAY-1436032 structure

CAS No.: 1803274-65-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 650.00	BP-02336-100mg	In stock	Get quote
250 mg	USD 1,250.00	BP-02336-250mg	In stock	Get quote
500 mg	USD 2,250.00	BP-02336-500mg	In stock	Get quote
1 g	Inquire	BP-02336-1g	In stock	Inquire
2 g	Inquire	BP-02336-2g	In stock	Inquire

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Description

BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.

Biological activity

BAY1436032 is a novel pan-mutant IDH1 inhibitor, it specifically inhibits R-2HG production and colony growth, and induces myeloid differentiation of AML cells. In vitro: BAY1436032 inhibited intracellular R-2HG production in mouse hematopoietic cells expressing IDH1R132H or IDH1R132C with an IC50 of 60 and 45 nm, respectively. In contrast, R-2HG levels were not reduced in IDH2R140Q and IDH2R172K expressing mouse hematopoietic cells by BAY1436032 at concentrations up to 10 μm. In vivo: Treatment with vehicle or 150 mg/kg BAY1436032 once daily by oral gavage was initiated at day 15 after transplantation. BAY1436032 and vehicle-treated mice had similar percentages of hCD45+ cells, peripheral blood counts, spleen weight at death and survival, confirming the on-target activity of BAY1436032

Identifiers

SMILES: C[C@H]1C[C@H](CC(C)(C)C1)N1C(NC2=CC=C(OC(F)(F)F)C=C2)=NC2=CC(CCC(O)=O)=CC=C12
InChIKey: RNMAUIMMNAHKQR-QFBILLFUSA-N

Specifications

MW (average): 489.5299
Formula: C₂₆H₃₀F₃N₃O₃
CAS No.: 1803274-65-8
Physical state: Solid
Color: white to grey
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4℃ 2 years; -20℃ 3 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Chaturvedi A, et al. Pan-mutant-IDH1 inhibitor BAY1436032 is highly effective against human IDH1 mutant acute myeloid leukemia in vivo. Leukemia. 2017 Oct;31(10):2020-2028.

Same target

Search Isocitrate Dehydrogenase (IDH)