| 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% |
| ALogP | 2.2 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CN(C)CC1=C(OC2=CC=CC=C21)C(=O)NCCOC3=CC=C(C=C3)C(=O)NO |
| 分子量 | 397.42 |
| Reaxy-Rn | 12075242 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12075242&ln= |
| 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); |
|---|
| 象形图 | GHS06, GHS08, GHS09, GHS05, GHS07 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H311: 皮肤接触有毒 H373: 通过长时间或反复暴露对器官造成损害 H411: 对水生生物有毒并具有长期持续影响 H314: 造成严重的皮肤灼伤和眼睛损伤 H302: 吞食有害 H318: 造成严重的眼睛损伤 H361: 怀疑破坏生育力或未出生的孩子 |
| 预防措施声明 |
P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P301+P330+P331: 如误吞咽：漱口。不要诱导呕吐。 P304+P340: 如误吸入：将人转移到空气新鲜处，保持呼吸舒适体位。 P363: 再次使用之前，请清洗受污染的衣物。 P391: 收集溢出物 P330: 漱口 P361+P364: 立即脱掉所有沾染的衣服，清洗后方可重新使用。 P203: 使用前，获取、阅读并遵守所有安全说明。 P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。 P301+P317: 如果被吞咽：请寻求医疗帮助。 P305+P354+P338: 如果进入眼睛：立即用水冲洗几分钟。取下隐形眼镜（如果有的话），并且操作简单。继续冲洗。 P318: 如果暴露或担心，请就医。 P317: 寻求紧急医疗救助。 P302+P361+P354: 如果接触皮肤：立即脱掉所有被污染的衣服。立即用水冲洗几分钟。 P316: 立即寻求紧急医疗救助。 P319: 如果你感到不适，请寻求医疗帮助。 |
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