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BAY-1436032

Cat. No. M6212
BAY-1436032 Structure
Size Price Availability Quantity
10mg USD 200 In stock
50mg USD 720 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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

Protocol
Cell Experiment
Cell lines HoxA9-IDH1R132 cell lines
Preparation method Vehicle or BAY1436032 was added to methylcellulose containing 105 human mononuclear cells, which were plated in duplicate. Colonies were evaluated microscopically 10 to 14 days after plating by standard criteria.
Concentrations 0.1 μm
Incubation time 24 h
Animal Experiment
Animal models NSG mice
Formulation DMSO
Dosages 45 or 150 mg/kg
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 489.53
Formula C26H30F3N3O3
CAS Number 1803274-65-8
Purity >99%
Solubility 10 mM in DMSO
Storage at -20°C
References

Pan-mutant-IDH1 inhibitor BAY1436032 is highly effective against human IDH1 mutant acute myeloid leukemia in vivo.
Chaturvedi A, et al. Leukemia. 2017 Oct;31(10):2020-2028. PMID: 28232670.

Pan-mutant IDH1 inhibitor BAY 1436032 for effective treatment of IDH1 mutant astrocytoma in vivo.
Pusch S, et al. Acta Neuropathol. 2017 Apr;133(4):629-644. PMID: 28124097.

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  Catalog
Abmole Inhibitor Catalog 2017




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