| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A408275-1ml |
1ml |
现货  |
|
| 别名 | 艾贝司他 (PCI-24781) |
|---|---|
| 英文别名 | CRA-024781 | 3-((dimethylamino)methyl)-N-(2-(4-(hydroxycarbamoyl)phenoxy)ethyl)benzofuran-2-carboxamide |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Abexinostat (PCI-24781) |
| 生化机理 | Abexinostat（PCI-24781，CRA-024781）是一种新型泛 HDAC 抑制剂，主要针对 HDAC1，Ki为 7 nM，对 HDAC 2、3、6 和 10 有适度的效力，对 HDAC8 的选择性超过 40 倍。1/2阶段。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 组蛋白去乙酰化酶抑制剂 |
| 产品介绍 |
PCI-24781 (Abexinostat)是一种新型的pan-HDAC抑制剂，靶向作用于HDAC1，Ki为7 nM，对HDACs 2， 3， 6，和10有适中的抑制性，但比作用于HDAC8选择性强40倍。An HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 inhibitor. Information Abexinostat (PCI-24781, CRA-024781) is a novel pan-HDAC inhibitor mostly targetingHDAC1withKiof 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2. PCI-24781 exhibits potent antitumor activity against a variety of tumor cell lines with GI50 ranging from 0.15 μM to 3.09 μM. PCI-24781 also has an antiproliferative effect on HUVEC endothelial cells with GI50 of 0.43 μM. PCI-24781 treatment causes dose-dependent accumulation of both acetylated histones and acetylated tubulin in HCT116 or DLD-1 cells, induces expression of p21, and leads to PARP cleavage and accumulation of the γH2AX. Inhibition of HDAC enzymes by PCI-24781 leads to a significant reduction in the transcription of genes specifically associated with HR, including RAD51. Consistent with inhibition of HR, PCI-24781 treatment results in a decreased ability to perform homology directed repair of I-SceI-induced chromosome breaks in transfected CHO cells. PCI-24781 induces S phase depletion, G2 cell cycle arrest, and apoptosis in soft tissue sarcoma (STS) cells. PCI-24781 induces Rad51 transcriptional repression in STS cells potentially mediated via enhanced E2F1 binding to the Rad51 proximal promoter. PCI-24781 induces caspase and reactive oxygen species-dependent apoptosis through NF-κB mechanisms in Hodgkin lymphoma and non-Hodgkin lymphoma cell lines. In vivo Administration of PCI-24781 at 200 mg/kg once daily every other day (q.o.d.) significantly inhibits the growth of HCT116 and DLD-1 xenografts in mice by 69% and 59%, respectively. Administration of PCI-24781 at 20 mg/kg, 40 mg/kg, 80 mg/kg, or 160 mg/kg once daily for 4 consecutive days followed by 3 days without treatment each week (q.d. × 4 per week) in the HCT116 model causes inhibition of tumor growth by 48%, 57%, 82.2%, or 80.0%, respectively. cell lines： Concentrations：Dissolved in DMSO, final concentrations ~10 μM Incubation Time：48, 72, 96, or 120 hours Powder Purity:≥95% |
| IC50 | HDAC8, IC50: 280 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CN(C)CC1=C(OC2=CC=CC=C12)C(=O)NCCOC3=CC=C(C=C3)C(=O)NO |
| 分子量 | 397.42 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 39 mg/mL (199.29 mM); Water: 39 mg/mL (199.29 mM); Ethanol: 39 mg/mL (199.29 mM); |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| NMR Spectrum 1H | Conforms to Structure |
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