CRA 24781
PCI-24781 (Abexinostat)
CAS: 783355-60-2
Molecular Formula: C21H23N3O5
CRA 24781 - Names and Identifiers
CRA 24781 - Physico-chemical Properties
| Molecular Formula | C21H23N3O5 |
| Molar Mass | 397.42 |
| Density | 1.284 |
| Melting Point | 198-202oC (dec.) |
| Solubility | DMSO (Slightly), Methanol (Slightly, Heated) |
| Appearance | Solid |
| Color | White |
| Storage Condition | Refrigerator |
| Use | Abexinostat (CRA 024781) is a new pan-HDAC inhibitor with a Ki value of 7 nM targeting HDAC1. |
| In vitro study | PCI-24781 have potent antitumor activity against a variety of tumor cell lines, GI50 is distributed between 0.15 μM and 3.09 μm. PCI-24781 also inhibited the proliferation of HUVEC endothelial cells with a GI50 of 0.43 μm. PCI-24781 treatment caused a dose-dependent accumulation of histone acetylation and tubulin acetylation in HCT116 and DLD-1 cell lines, while inducing p21 expression, cleavage of PARP, and accumulation of γH2AX. PCI-24781 inhibition of HDACs enzyme activity led to a significant decrease in the transcription level of HR related genes, including rad51. Consistent with inhibition of HR, in CHO cells, PCI-24781 treatment resulted in a decrease in homology-directed repair capacity I-SceI to induced chromatin breaks. PCI-24781 induces S-phase deletion, G2-phase cell cycle arrest, and apoptosis of soft tissue (STS) cells. PCI-24781 induced transcriptional repression of Rad51 in STS cells is likely to be by enhancing the binding of E2F1 in the proximal promoter region of rad51. PCI-24781 also induces a protease-and reactive oxygen species-dependent NF-κB signaling pathway-mediated apoptotic process in Hodgkin's lymphoma and non-Hodgkin's lymphoma. |
| In vivo study | PCI-24781 at a dose of 200 mg/kg in transplanted mice once a day significantly inhibited the growth of HCT116 and DLD-1 tumor cells by 69% and 59%, respectively. PCI-24781 were administered at 20 mg/kg, 40 mg/kg, 80 mg/kg and 160 mg/kg for four consecutive days per week, after three days of no treatment (once a day, four days a week) in the HCT116 transplanted mouse model, the inhibitory effects were 48%, 57%, 82.2, and 80.0, respectively. |
CRA 24781 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.516 ml | 12.581 ml | 25.162 ml |
| 5 mM | 0.503 ml | 2.516 ml | 5.032 ml |
| 10 mM | 0.252 ml | 1.258 ml | 2.516 ml |
| 5 mM | 0.05 ml | 0.252 ml | 0.503 ml |
Last Update：2024-01-02 23:10:35
CRA 24781 - Reference Information
| biological activity | Abexinostat (PCI-24781, CRA-024781) is a novel pan-HDAC inhibitor targeting HDAC1, the Ki is 7 nM and is moderately inhibitory to HDACs 2, 3, 6, and 10, but is 40-fold more selective than hdac8. Phase 1/2. |
| Target | Value |
| HDAC1 (Cell-free assay) | 7 nM(Ki) |
| HDAC3/SMRT | 8.2 nM(Ki) |
| HDAC6 | 17 nM(Ki) |
| HDAC2 (Cell-free assay) | 19 nM(Ki) |
| HDAC10 | 24 nM |
| Use | PCI-24781 is a novel hydraulic acid HDAC inhibitor. PCI-24781 exerts cytotoxicity and histone H3 alterations via caspase-8 and FADD in leucemia cells. |
Last Update：2024-04-09 20:02:46
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Spot supply
Product Name: PCI-24781 (Abexinostat) Visit Supplier Webpage Request for quotationCAS: 783355-60-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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