N,N-Dicyclopropyl-4-((1,5-dimethyl-1H-pyrazol-3-yl)amino)-6-ethyl-1-methyl-1,6-dihydroimidazo[
BMS 911543
CAS: 1271022-90-2
Molecular Formula: C23H28N8O
N,N-Dicyclopropyl-4-((1,5-dimethyl-1H-pyrazol-3-yl)amino)-6-ethyl-1-methyl-1,6-dihydroimidazo[ - Names and Identifiers
N,N-Dicyclopropyl-4-((1,5-dimethyl-1H-pyrazol-3-yl)amino)-6-ethyl-1-methyl-1,6-dihydroimidazo[ - Physico-chemical Properties
| Molecular Formula | C23H28N8O |
| Molar Mass | 432.52 |
| Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
| In vitro study | BMS-911543 in SET-2 and BaF3-V617F cell lines, with potent antiproliferative activity (IC50 60 nM and 70 nM, respectively). This activity is associated with inhibition of the persistently activated pSTAT5 activity. In contrast, non-jak2-dependent cell lines such as A549, MDA-MB-231, MiaPaCa-2 significantly less sensitive to treatment with the inhibitor. Cell lines dependent on other JAK family members, including CTLL2 and IL-3-stimulated BaF3 cells, have weak antiproliferative activity against BMS-911543 (IC50 2.9 and 3.5 μm, respectively). |
| In vivo study | BMS-911543 suppressed pSTAT5 levels in a mouse model stimulated with thrombopoietin (TPO). This response was dose-dependent, resulting in a complete return to normal pSTAT5 levels at the highest oral dose of 30 mg/kg, which was maintained for 18 hours. At a moderate oral dose of 10 mg/kg, pSTAT5 levels were reduced by 65%; Instead, at a dose of 5 mg/kg, pSTAT5 levels were reduced by 50% and maintained for 8 hours. The observed decrease in pSTAT5 was associated with BMS-911543 treatment, with AUC0-8h of 23, 41 and 109 μm · h at 5, 10 and 30 mg/kg, respectively. The absolute oral bioavailability of BMS-911543 in liquid form is greater than 50% in mice, rats, dogs and monkeys. In addition, the absorption of BMS-911543 is not significantly affected by the particle lysate (suspension formulation), and its relative oral bioavailability (ratio of suspension to liquid) in rats is about 60%; In dogs, its relative oral bioavailability is almost 100%. |
N,N-Dicyclopropyl-4-((1,5-dimethyl-1H-pyrazol-3-yl)amino)-6-ethyl-1-methyl-1,6-dihydroimidazo[ - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.312 ml | 11.56 ml | 23.12 ml |
| 5 mM | 0.462 ml | 2.312 ml | 4.624 ml |
| 10 mM | 0.231 ml | 1.156 ml | 2.312 ml |
| 5 mM | 0.046 ml | 0.231 ml | 0.462 ml |
Last Update：2024-01-02 23:10:35
N,N-Dicyclopropyl-4-((1,5-dimethyl-1H-pyrazol-3-yl)amino)-6-ethyl-1-methyl-1,6-dihydroimidazo[ - Reference Information
| biological activity | BMS-911543 is a potent, selective small molecule inhibitor of JAK2 with an IC50 of 1.1 nM. |
| Target | Value |
| JAK2 (Cell-free assay) | 1.1 nM |
| SET-2 (Cell-free assay) | 60 nM |
| TYK2 (Cell-free assay) | 66 nM |
| JAK3 (Cell-free assay) | 75 nM |
Last Update：2024-04-09 15:16:56
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Product Name: BMS 911543 Visit Supplier Webpage Request for quotation
CAS: 1271022-90-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1271022-90-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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