CS-1736
GSK1324726A
CAS: 1300031-52-0
Molecular Formula: C25H23ClN2O3
CS-1736 - Names and Identifiers
CS-1736 - Physico-chemical Properties
| Molecular Formula | C25H23ClN2O3 |
| Molar Mass | 434.91 |
| Density | 1.304±0.06 g/cm3(Predicted) |
| Boling Point | 707.3±60.0 °C(Predicted) |
| Solubility | DMSO : ≥ 46 mg/mL (105.77 mM) |
| pKa | 4.20±0.10(Predicted) |
| Storage Condition | -20℃ |
| Use | GSK1324726A is a potent selective BET protein inhibitor with high affinity binding to BRD2 (IC50=41 nM),BRD3 (IC50=31 nM) and BRD4 (IC50=22 nM). |
| Target | BRD2; BRD3; BRD4 |
| In vitro study | In neuroblastoma cell lines, GSK1324726A inhibits cell growth and induces cytotoxicity. GSK1324726A also modulates expression of genes involved in apoptosis, signaling, and MYC-family pathways, including the direct suppression of BCL2 and MYCN. |
| In vivo study | In the mouse SK–N-AS and CHP-212 models, GSK1324726A (15 mg/kg p.o.) results in tumor growth inhibition and down-regulation MYCN and BCL2 expression. In a mouse septic shock model, GSK1324726A (10 mg/kg i.v.) shows potent anti-inflammatory effects, and prevents death of diseased animals. |
CS-1736 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.299 ml | 11.497 ml | 22.993 ml |
| 5 mM | 0.46 ml | 2.299 ml | 4.599 ml |
| 10 mM | 0.23 ml | 1.15 ml | 2.299 ml |
| 5 mM | 0.046 ml | 0.23 ml | 0.46 ml |
Last Update：2024-01-02 23:10:35
CS-1736 - Reference Information
| biological activity | GSK1324726A(I-BET726) is a highly selective inhibitor of BET family proteins. the IC50 for BRD2, BRD3, and BRD4 is 41 nM, 31 nM, and 22 nM respectively. |
| in vitro studies | in neuroblastoma cell lines, GSK1324726A inhibits cell growth and induces cytotoxicity. GSK1324726A also modulates expression of genes involved in apoptosis, signaling, and MYC-family pathways, including the direct suppression of BCL2 and MYCN. |
| in vivo research | in the mouse SK-N-AS and CHP-212 models, GSK1324726A (15 mg/kg p.o.) results in tumor growth inhibition and down-regulation MYCN and BCL2 expression. In a mouse septic shock model, GSK1324726A (10 mg/kg I. v.) shows potent anti-inflammatory effects, and prevents death of diseased animals. |
Last Update：2024-04-09 21:54:55
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