BAY-1436032
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $1350 | Check With Us |
| 500mg | $2050 | Check With Us |
| 1g | $3075 | Check With Us |
: Cat #: V4174 CAS #: 1803274-65-8 Purity ≥ 98%
Description: BAY-1436032 is a novel and potent pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor both in vitro and in vivo.
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| Molecular Weight (MW) | 489.53 |
|---|---|
| Molecular Formula | C26H30F3N3O3 |
| CAS No. | 1803274-65-8 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| SMILES Code | O=C(O)CCC1=CC=C2N([C@H]3CC(C)(C)C[C@@H](C)C3)C(NC4=CC=C(OC(F)(F)F)C=C4)=NC2=C1 |
| Synonyms | BAY-1436032; BAY 1436032; BAY1436032 |
| Protocol | 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. |
|---|---|---|
| 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.0428 mL | 10.2139 mL | 20.4278 mL | 40.8555 mL |
| 5mM | 0.4086 mL | 2.0428 mL | 4.0856 mL | 8.1711 mL |
| 10mM | 0.2043 mL | 1.0214 mL | 2.0428 mL | 4.0856 mL |
| 20mM | 0.1021 mL | 0.5107 mL | 1.0214 mL | 2.0428 mL |
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