Size | Price | Stock |
---|---|---|
5mg | $90 | In-stock |
10mg | $150 | In-stock |
25mg | $340 | In-stock |
50mg | $570 | In-stock |
100mg | $980 | In-stock |
200 mg | Get quote | |
500 mg | Get quote | |
We match the lowest price on market. |
We offer a substantial discount on larger orders, please inquire via [email protected]
or Fax: (86)21-58955996
Inquiry for price and availability only. Please place your order via our email or fax.
Cat. No. : | HY-100020 |
M.Wt: | 489.53 |
Formula: | C26H30F3N3O3 |
Purity: | >98 % |
Solubility: | DMSO : 125 mg/mL (255.35 mM; Need ultrasonic and warming) |
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].
Lorem ipsum dolor sit amet, consectetur adipisicing elit. Autem earum hic iste maiores, nam neque rem suscipit. Adipisci consequatur error exercitationem fugit ipsam optio qui, quibusdam repellendus sed vero! Debitis.
Inquiry Information
Your information is safe with us.