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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Abexinostat (PCI-24781), 组蛋白去乙酰化酶抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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.
In vitro
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 Data
cell lines：
Concentrations：Dissolved in DMSO, final concentrations ~10 μM
Incubation Time：48, 72, 96, or 120 hours
Powder Purity:≥95%
规格
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。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
组蛋白去乙酰化酶抑制剂
名称和识别符
EC号
811-183-9
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=
技术文档
高级数据
产品属性
| ALogP | 2.2 |
|---|
关联靶点（人）
HDAC4
Tclin
组蛋白去乙酰化酶4(Histone deacetylase 4)
(1 活性数据)
HDAC6
Tclin
组蛋白去乙酰化酶6(Histone deacetylase 6)
(3 活性数据)
HDAC1
Tclin
组蛋白去乙酰化酶1(Histone deacetylase 1)
(4 活性数据)
HDAC7
Tclin
组蛋白去乙酰化酶7(Histone deacetylase 7)
(1 活性数据)
HDAC11
Tclin
组蛋白去乙酰化酶11(Histone deacetylase 11)
(1 活性数据)
HDAC9
Tclin
组蛋白去乙酰化酶9(Histone deacetylase 9)
(1 活性数据)
HDAC2
Tclin
组蛋白去乙酰化酶2(Histone deacetylase 2)
(3 活性数据)
HDAC10
Tclin
组蛋白去乙酰化酶10(Histone deacetylase 10)
(5 活性数据)
HDAC8
Tclin
组蛋白去乙酰化酶8(Histone deacetylase 8)
(3 活性数据)
HDAC5
Tclin
组蛋白去乙酰化酶5(Histone deacetylase 5)
(1 活性数据)
HDAC3
Tclin
组蛋白去乙酰化酶3(Histone deacetylase 3)
(3 活性数据)
化学和物理性质
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);
安全和危险性（GHS）
信号词
危险
危险声明
H302: 吞食有害
H311: 皮肤接触有毒
H314: 造成严重的皮肤灼伤和眼睛损伤
H411: 对水生生物有毒并具有长期持续影响
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 L2214609 |
分析证书 | A408275 |
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