1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)
  3. BAY-1436032

BAY-1436032 

Cat. No.: HY-100020 Purity: 98.94%
Handling Instructions

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

For research use only. We do not sell to patients.

BAY-1436032 Chemical Structure

BAY-1436032 Chemical Structure

CAS No. : 1803274-65-8

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 176 In-stock
Estimated Time of Arrival: December 31
5 mg USD 160 In-stock
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10 mg USD 260 In-stock
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25 mg USD 590 In-stock
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50 mg USD 990 In-stock
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100 mg USD 1780 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

IDH1[1]

In Vitro

BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor. BAY-1436032 inhibits intracellular (R)-2-hydroxyglutarate (R-2HG) production in mouse hematopoietic cells expressing IDH1R132H or IDH1R132C with IC50s of 60 and 45 nM, respectively. 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[1].

In Vivo

Long-term exposure to once daily oral BAY-1436032 reveals nearly complete suppression of (R)-2-hydroxyglutarate (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 compare to the 150 mg/kg cohort at day 60, while platelet counts are significantly reduced in vehicle and 45 mg/kg BAY-1436032 treated mice compare 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 (P<0.001), 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[1].

Clinical Trial
Molecular Weight

489.53

Formula

C₂₆H₃₀F₃N₃O₃

CAS No.

1803274-65-8

SMILES

O=C(O)CCC1=CC=C2C(N=C(NC3=CC=C(OC(F)(F)F)C=C3)N2[[email protected]]4CC(C)(C)C[[email protected]@H](C)C4)=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (255.35 mM; Need ultrasonic and warming)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0428 mL 10.2139 mL 20.4278 mL
5 mM 0.4086 mL 2.0428 mL 4.0856 mL
10 mM 0.2043 mL 1.0214 mL 2.0428 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.11 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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 105 human mononuclear cells, which are plated in duplicate. Colonies are evaluated microscopically 10 to 14 days after plating by standard criteria[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 98.94%

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Product Name:
BAY-1436032
Cat. No.:
HY-100020
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