Abexinostat | 阿贝司他 | Pci-24781 | HDAC/MBLAC2 Inhibitor

首页 / 抑制剂/激动剂 / / 组蛋白去乙酰化酶 / Abexinostat/艾贝司他

Abexinostat/艾贝司他 {[allProObj[0].p_purity_real_show]}

货号：A195616 同义名： 阿贝司他 / Pci-24781; CRA 024781

PCI-24781 is a 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.

Abexinostat/艾贝司他化学结构
CAS号：783355-60-2

Abexinostat/艾贝司他 3D分子结构
CAS号：783355-60-2

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price) ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price) ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]}	现货	1周咨询	- +

购物车0 收藏询单

sales@ambeed.cn tech@ambeed.cn 400-920-2911 产品手册产品订购技术咨询
快速发货顺丰冷链运输，1-2 天到达

品质保证

技术支持

免费溶解

Abexinostat/艾贝司他纯度/质量文件产品仅供科研

货号：A195616 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: 更多 >

组蛋白去乙酰化酶亚型比较

产品名称	HD1 ↓ ↑	HD2 ↓ ↑	HDAC ↓ ↑	HDAC1 ↓ ↑	HDAC10 ↓ ↑	HDAC11 ↓ ↑	HDAC2 ↓ ↑	HDAC3 ↓ ↑	HDAC4 ↓ ↑	HDAC5 ↓ ↑	HDAC6 ↓ ↑	HDAC7 ↓ ↑	HDAC8 ↓ ↑	HDAC9 ↓ ↑	其他靶点	纯度
Givinostat HCl monohydrate	++++ HD1-A, IC50: 16 nM HD1-B, IC50: 7.5 nM	+++ HD2, IC50: 10 nM														99%+
MC1568	++ HD1-B (Maize), IC50: 3.4 μM HD1-A (Maize), IC50: 100 nM															96%
Trichostatin A			++++ HDAC, IC50: ~1.8 nM													99%+
Scriptaid			✔													99%+
Valproic acid sodium			✔												Autophagy	97%
AR-42			+++ HDAC, IC50: 30 nM													99%+
Dacinostat			+++ HDAC, IC50: 32 nM													98+%
CUDC-101			++++ HDAC, IC50: 4.4 nM	++++ HDAC1, IC50: 4.5 nM	+++ HDAC10, IC50: 26.1 nM			++++ HDAC3, IC50: 9.1 nM	+++ HDAC4, IC50: 13.2 nM	+++ HDAC5, IC50: 11.4 nM		+ HDAC7, IC50: 373 nM	++ HDAC8, IC50: 79.8 nM	++ HDAC9, IC50: 67.2 nM	HER2,EGFR	99%+
M344			++ HDAC, IC50: 100 nM													99%+
Splitomicin			+ Sir2p, IC50: 60 μM													99%
Panobinostat			++++ HDAC (MOLT-4 cells), IC50: 5 nM HDAC (Reh cells), IC50: 20 nM													98%
Sodium 4-Phenylbutyrate			✔													98%
Vorinostat			+++ HDAC, IC50: ~10 nM													98%
Curcumin			✔												Nrf2,NF-κB	98%
Belinostat			+++ HDAC, IC50: 27 nM													98%
RG-2833				++ HDAC1, Ki: 32 nM				++ HDAC3, Ki: 5 nM								98%
Valproic acid				+ HDAC1, IC50: 0.4 mM												98%
BG45				+ HDAC1, IC50: 2 μM			+ HDAC2, IC50: 2.2 μM	+ HDAC3, IC50: 289 nM								99%+
Entinostat				+ HDAC1, IC50: 0.51 μM				+ HDAC3, IC50: 1.7 μM								98%
Resminostat				+++ HDAC1, IC50: 42.5 nM				++ HDAC3, IC50: 50.1 nM			++ HDAC6, IC50: 71.8 nM					98+%
Romidepsin				+++ HDAC1, IC50: 36 nM			+++ HDAC2, IC50: 47 nM									99%+
Parthenolide				✔											NF-κB,p53	97% HPLC
Tacedinaline				+ HDAC1, IC50: 0.9 μM			+ HDAC2, IC50: 0.9 μM	+ HDAC3, IC50: 1.2 μM								98%
Mocetinostat				++ HDAC1, IC50: 0.15 μM		+ HDAC11, IC50: 0.59 μM	+ HDAC2, IC50: 0.29 μM	+ HDAC3, IC50: 1.66 μM								98%
WT-161				++++ HDAC1, IC50: 8.35 nM			+++ HDAC2, IC50: 15.4 nM				++++ HDAC6, IC50: 0.4 nM					99%+
Fimepinostat				++++ HDAC1, IC50: 1.7 nM	++++ HDAC10, IC50: 2.8 nM	++++ HDAC11, IC50: 5.4 nM		++++ HDAC3, IC50: 1.8 nM			+++					99%+
Tucidinostat				++ HDAC1, IC50: 95 nM	++ HDAC10, IC50: 78 nM		++ HDAC2, IC50: 160 nM	++ HDAC3, IC50: 67 nM								99%+
Santacruzamate A							++++ HDAC2, IC50: 119 pM									99%+
(E,E)-RGFP966								++ HDAC3, IC50: 80 nM								99%+
LMK-235									+++ HDAC4, IC50: 11.9 nM	++++ HDAC5, IC50: 4.2 nM						99%+
Tasquinimod									✔							99%+
CAY10603											++++ HDAC6, IC50: 2 pM					98%
Tubastatin A											+++ HDAC6, IC50: 15 nM					98%
Tubacin											++++ HDAC6, IC50: 4 nM					99%+
ACY-738											++++ HDAC6, IC50: 1.7 nM					99%+
Nexturastat A											++++ HDAC6, IC50: 5 nM					99%+
BRD73954											+++ HDAC6, IC50: 36 nM		++ HDAC8, IC50: 120 nM			99%
Tubastatin A HCl											+++ HDAC6, IC50: 15 nM		+ HDAC8, IC50: 854 nM			98%
PCI-34051													+++ HDAC8, IC50: 10 nM			99%+
Ricolinostat				++ HDAC1, IC50: 58 nM			++ HDAC2, IC50: 48 nM	++ HDAC3, IC50: 51 nM			++++ HDAC6, IC50: 4.7 nM		++ HDAC8, IC50: 100 nM			99%+
Droxinostat								+ HDAC3, IC50: 16.9 μM			+ HDAC6, IC50: 2.47 μM		+ HDAC8, IC50: 1.46 μM			99%+
Abexinostat				++++ HDAC1, Ki: 7 nM	+++ HDAC10, IC50: 24 nM		+++ HDAC2, Ki: 19 nM	++++ HDAC3/SMRT, Ki: 8.2 nM			+++ HDAC6, Ki: 17 nM		+ HDAC8, IC50: 280 nM			98%+
Citarinostat				+++ HDAC1, IC50: 35 nM			+++ HDAC2, IC50: 45 nM	+++ HDAC3, IC50: 46 nM			++++ HDAC6, IC50: 2.6 nM		++ HDAC8, IC50: 137 nM			99%+
HPOB				+ HDAC1, IC50: 2.9 μM	+ HDAC10, IC50: 3.0 μM			+ HDAC3, IC50: 1.7 μM					+ HDAC8, IC50: 2.8 μM			97%
Quisinostat 2HCl				++++ HDAC1, IC50: 0.11 nM	++++ HDAC10, IC50: 0.46 nM	++++ HDAC11, IC50: 0.37 nM	++++ HDAC2, IC50: 0.33 nM	++++ HDAC3, IC50: 4.86 nM	++++ HDAC4, IC50: 0.64 nM	++++ HDAC5, IC50: 3.69 nM			++++ HDAC8, IC50: 4.26 nM			97%
Domatinostat				+ HDAC1, IC50: 1.20 μM	+ HDAC10, IC50: 21 μM	+ HDAC11, IC50: 9.7 μM								+ HDAC9, IC50: 50 μM		99%+
TMP269									++ HDAC4, IC50: 157 nM	++ HDAC5, IC50: 97 nM		+++ HDAC7, IC50: 43 nM		+++ HDAC9, IC50: 23 nM		99%+
Pracinostat				++ HDAC1, IC50: 49 nM	+++ HDAC10, IC50: 40 nM							++ HDAC7, IC50: 137 nM	++ HDAC8, IC50: 140 nM	++ HDAC9, IC50: 70 nM		99%+
TMP195									++ HDAC4, Ki: 59 nM	++ HDAC5, Ki: 60 nM		+++ HDAC7, Ki: 26 nM		+++ HDAC9, Ki: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Abexinostat/艾贝司他生物活性

靶点	HDAC8 HDAC8, IC50:280 nM HDAC8 HDAC8, IC50:280 nM HDAC8 HDAC8, IC50:280 nM HDAC8 HDAC8, IC50:280 nM
描述	PCI-24781 is a novel hydroxamic acid–based pan-HDAC inhibitor with Ki values of 7nM, 19nM, 8.2nM, 17nM, 280nM and 24nM for HDAC1 HDAC2, HDAC3/SMRT, HDAC6, HDAC8 and HDAC10. Treatment with PCI-24781 at concentration ranging in 0.5-10μM resulted in the accumulation of acetylated histone and acetylated tubulin in a dose-dependent manner, accompanied with increase of p21, and resulted in an inhibition of tumor cell growth and the induction of apoptosis shown by increased γH2AX and cleaved PARP in HCT116, DLD-1 and HUVEC cells. Administration of PCI-24781 (i.v., formulated in 30% HP-cyclodextrin) to mice harboring HCT116 or DLD-1 colon tumor xenografts resulted in a statistically significant reduction in tumor growth. Inhibition of HDAC enzymes by PCI-24781 led to a significant reduction in the transcription of genes specifically associated with HR, including RAD51. RAD51 protein levels were significantly decreased after 24 h of drug exposure both in vitro and in vivo.
作用机制	PCI-24781 is a hydroxamic acid–based inhibitor which can chelate the Zn²⁺ of HDAC.^[1]

Abexinostat/艾贝司他动物研究

Dose

Mice: 12.5 mg/kg^[3] (i.p.), 50 mg/kg^[4] (i.p.) Nude Mice: 10 mg/kg - 200 mg/kg^[1] (i.v.)

Administration

i.p., i.v.

Pharmacokinetics

Animal	Nude mice^[1]
Dose	10 mg/kg
Administration	i.v.
T_1/2	6.7 min
CL	297 ml/min/kg

Abexinostat/艾贝司他参考文献

[1]Buggy JJ, Cao ZA, et al. CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo. Mol Cancer Ther. 2006 May;5(5):1309-17.

[2]Adimoolam S, Sirisawad M, et al. HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19482-7. Epub 2007 Nov 27.

[3]Sholler GS, Currier EA, et al. PCI-24781 (abexinostat), a novel histone deacetylase inhibitor, induces reactive oxygen species-dependent apoptosis and is synergistic with bortezomib in neuroblastoma. J Cancer Ther Res. 2013 Dec 28;2:21.

[4]Lopez G, Liu J, et al. Combining PCI-24781, a novel histone deacetylase inhibitor, with chemotherapy for the treatment of soft tissue sarcoma. Clin Cancer Res. 2009 May 15;15(10):3472-83.

Abexinostat/艾贝司他实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.58mL

2.52mL

1.26mL

25.16mL

5.03mL

2.52mL

Abexinostat/艾贝司他技术信息

CAS号	783355-60-2
分子式	C₂₁H₂₃N₃O₅
分子量	397.42
SMILES Code	O=C(C1=C(CN(C)C)C2=CC=CC=C2O1)NCCOC3=CC=C(C(NO)=O)C=C3
MDL No.	MFCD10565969

别名	阿贝司他 ;Pci-24781; CRA 024781; CRA-24781
运输	蓝冰
InChI Key	MAUCONCHVWBMHK-UHFFFAOYSA-N
Pubchem ID	11749858

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

动物实验：配制的工作液建议现用现配，短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

Abexinostat/艾贝司他 {[allProObj[0].p_purity_real_show]}

Abexinostat/艾贝司他纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Abexinostat/艾贝司他质控信息

Abexinostat/艾贝司他生物活性

Abexinostat/艾贝司他动物研究

Abexinostat/艾贝司他参考文献

Abexinostat/艾贝司他实验方案

Abexinostat/艾贝司他技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

HDAC8	HDAC8, IC50:280 nM
HDAC8	HDAC8, IC50:280 nM
HDAC8	HDAC8, IC50:280 nM
HDAC8	HDAC8, IC50:280 nM
HDAC10	HDAC10, IC50:24 nM
HDAC10	HDAC10, IC50:24 nM
HDAC10	HDAC10, IC50:24 nM
HDAC10	HDAC10, IC50:24 nM
HDAC1	HDAC1, Ki:7 nM
HDAC1	HDAC1, Ki:7 nM
HDAC1	HDAC1, Ki:7 nM
HDAC1	HDAC1, Ki:7 nM
HDAC3	HDAC3/SMRT, Ki:8.2 nM
HDAC3	HDAC3/SMRT, Ki:8.2 nM
HDAC3	HDAC3/SMRT, Ki:8.2 nM
HDAC3	HDAC3/SMRT, Ki:8.2 nM
HDAC6	HDAC6, Ki:17 nM
HDAC6	HDAC6, Ki:17 nM
HDAC6	HDAC6, Ki:17 nM
HDAC6	HDAC6, Ki:17 nM
HDAC2	HDAC2, Ki:19 nM
HDAC2	HDAC2, Ki:19 nM
HDAC2	HDAC2, Ki:19 nM
HDAC2	HDAC2, Ki:19 nM

Abexinostat/艾贝司他 {[allProObj[0].p_purity_real_show]}

Abexinostat/艾贝司他 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Abexinostat/艾贝司他 质控信息

Abexinostat/艾贝司他 生物活性

Abexinostat/艾贝司他 动物研究

Abexinostat/艾贝司他 参考文献

Abexinostat/艾贝司他 实验方案

Abexinostat/艾贝司他 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

Abexinostat/艾贝司他纯度/质量文件产品仅供科研

Abexinostat/艾贝司他质控信息

Abexinostat/艾贝司他生物活性

Abexinostat/艾贝司他动物研究

Abexinostat/艾贝司他参考文献

Abexinostat/艾贝司他实验方案

Abexinostat/艾贝司他技术信息