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PCI-24781(Abexinostat),广谱组蛋白去酰基化酶(HDAC)抑制剂, 组蛋白去乙酰化酶抑制剂

广谱组蛋白去酰基化酶(HDAC)抑制剂。
规格或纯度: ≥97%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
P126975-1mg
1mg 现货 Stock Image
P126975-5mg
5mg 现货 Stock Image
P126975-10mg
10mg 现货 Stock Image
P126975-50mg
50mg 现货 Stock Image

基本描述

英文别名 ABEXINOSTAT|783355-60-2|PCI-24781|PCI 24781|CRA-024781|CRA 024781|CRA-02478|3-((dimethylamino)methyl)-N-(2-(4-(hydroxycarbamoyl)phenoxy)ethyl)benzofuran-2-carboxamide|PCI24781|CRA 24781|Abexinostat [USAN]|Abexinostat (PCI-24781)|PCI-24781 (Abexinostat)|S7
规格或纯度 ≥97%
英文名称 PCI-24781 (Abexinostat)
生化机理 PCI-24781 is a broad spectrum hydroxamic acid-based inhibitor of HDAC that shows antitumor activity in vitro. PCI-24781 inhibited pure recombinant HDAC1 with a Ki of 0.007 Mmol/L, as well as HDAC2, HDAC3/SMRT, HDAC6, HDAC8, and HDAC10 in the nanomolar range. Antitumor activity of PCI-24781 was observed in all 10 tumor cell lines tested, with GI50% values ranging from 0.15 to 3.09 μmol/L.Broad spectrum phenyl hydroamic acid inhibitor of HDAC (histone deacetylase). Nanomolar potency in cell-free assays (HDAC1 K i = 7nM; HDAC2 K i = 19 nM; HDAC3 K i = 8.2 nM; HDAC6 K i = 17nM; HDAC8 IC 50 = 280 nM; HDAC10 IC 50 = 24 nM). Inhibits several is
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 有毒,请参阅SDS以获取更多信息。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
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.

PCI-24781 (Abexinostat) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8.
An HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 inhibitor.

产品属性

ALogP 2.2

名称和标识符

IUPAC Name 3-[(dimethylamino)methyl]-N-[2-[4-(hydroxycarbamoyl)phenoxy]ethyl]-1-benzofuran-2-carboxamide
INCHI InChI=1S/C21H23N3O5/c1-24(2)13-17-16-5-3-4-6-18(16)29-19(17)21(26)22-11-12-28-15-9-7-14(8-10-15)20(25)23-27/h3-10,27H,11-13H2,1-2H3,(H,22,26)(H,23,25)
InChi Key MAUCONCHVWBMHK-UHFFFAOYSA-N
Canonical SMILES CN(C)CC1=C(OC2=CC=CC=C21)C(=O)NCCOC3=CC=C(C=C3)C(=O)NO
Isomeric SMILES CN(C)CC1=C(OC2=CC=CC=C21)C(=O)NCCOC3=CC=C(C=C3)C(=O)NO
PubChem CID 11749858
分子量 397.42

化学和物理性质

溶解性 DMSO ≥78mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

安全和危险性(GHS)

象形图
ghs06

Toxic

ghs08

Health Hazard

ghs09

Environmental Hazard

ghs05

Corrosive

ghs07

Harmful

信号词 Danger
危险声明 H311: Toxic in contact with skin
H373: Causes damage to organs through prolonged or repeated exposure
H411: Toxic to aquatic life with long lasting effects
H314: Causes severe skin burns and eye damage
H302: Harmful if swallowed
H318: Causes serious eye damage
H361: Suspected of damaging fertility or the unborn child
预防措施声明 P273,P280,P302+P352,P321,P405,P501,P264,P260,P270,P301+P330+P331,P304+P340,P363,P391,P330,P361+P364,P203,P264+P265,P301+P317,P305+P354+P338,P318,P317,P302+P361+P354,P316,P319

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参考文献

1. Buggy JJ, Cao ZA, Bass KE, Verner E, Balasubramanian S, Liu L, Schultz BE, Young PR, Dalrymple SA.  (2006)  CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo..  Mol Cancer Ther,  (5):  (1309-17).  [PMID:16731764]
2. Liu L, Chen B, Qin S, Li S, He X, Qiu S, Zhao W, Zhao H.  (2010)  A novel histone deacetylase inhibitor Chidamide induces apoptosis of human colon cancer cells..  Biochem Biophys Res Commun,  392  (2):  (190-5).  [PMID:20060381]
3. Mithraprabhu S, Grigoriadis G, Khong T, Spencer A.  (2010)  Deactylase inhibition in myeloproliferative neoplasms..  Invest New Drugs,  28 Suppl 1  (13):  (S50-7).  [PMID:21127942]
4. Prebet T, Vey N.  (2011)  Vorinostat in acute myeloid leukemia and myelodysplastic syndromes..  Expert Opin Investig Drugs,  20  (2):  (287-95).  [PMID:21192773]