貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S80950-2mg	96.7%	￥360.00 S80950-2mg ￥360.00 現(xiàn)貨	8 8	-	-	-
S80950-5mg	96.7%	￥520.00 S80950-5mg ￥520.00 現(xiàn)貨	6 6	-	-	-
S80950-10mg	96.7%	￥800.00 S80950-10mg ￥800.00 現(xiàn)貨	6 6	-	-	-
S80950-25mg	96.7%	￥1280.00 S80950-25mg ￥1280.00 現(xiàn)貨	6 6	-	-	-
S80950-100mg	96.7%	￥3840.00 S80950-100mg ￥3840.00 現(xiàn)貨	2 2	-	-	-

產(chǎn)品介紹

Abexinostat (CRA 024781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM. Abexinostat also inhibits metallo-β-lactamase domain-containing protein?2 (MBLAC2) hydrolase activity with an EC50 below 10 nM

產(chǎn)品描述：

靶點(diǎn)：

HDAC1:7 nM (Ki);HDAC3/SMRT:8.2 nM (Ki);HDAC6:17 nM (Ki);HDAC2:19 nM (Ki);HDAC10:24 nM (Ki);HDAC8:280 nM (Ki);MBLAC2:<10 nM (EC50);HDAC

體外研究：

Abexinostat (CRA 024781) exhibits potent antitumor activity against a variety of tumor cell lines with GI50% ranging from 0.15 μM to 3.09 μM. Abexinostat (CRA 024781) also has an antiproliferative effect on HUVEC endothelial cells with GI50% of 0.43 μM. Abexinostat (CRA 024781) 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[1]. Inhibition of HDAC enzymes by Abexinostat (CRA 024781) leads to a significant reduction in the transcription of genes specifically associated with HR, including RAD51. Consistent with inhibition of HR, Abexinostat (CRA 024781) treatment results in a decreased ability to perform homology directed repair of I-SceI-induced chromosome breaks in transfected CHO cells[2]. Abexinostat (CRA 024781) induces S phase depletion, G2 cell cycle arrest, and apoptosis in soft tissue sarcoma (STS) cells. Abexinostat (CRA 024781) induces Rad51 transcriptional repression in STS cells potentially mediated via enhanced E2F1 binding to the Rad51 proximal promoter.

體內(nèi)研究：

Abexinostat (CRA 024781) parenterally administered to mice harboring HCT116 or DLD-1 colon tumor xenografts results in a statistically significant reduction in tumor growth. Inhibition of tumor growth is accompanied by an increase in the acetylation of α-tubulin in peripheral blood mononuclear cells, and an alteration in the expression of many genes in the tumors, including several involved in apoptosis and cell growth。

參考文獻(xiàn)：

1. Buggy JJ, et al. CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo. Mol Cancer Ther, 2006, 5(5), 1309-1317. 2. Adimoolam S, et al. HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination. Proc Natl Acad Sci U S A, 2007, 104(49), 19482-19487. 3. Lopez G, et al. Combining PCI-24781, a novel histone deacetylase inhibitor, with chemotherapy for the treatment of soft tissue sarcoma. Clin Cancer Res, 2009, 15(10), 3472-3483. 4. Lechner S, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Aug;18(8):812-820.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.516 ml	12.581 ml	25.162 ml
5 mM	0.503 ml	2.516 ml	5.032 ml
10 mM	0.252 ml	1.258 ml	2.516 ml
50 mM	0.05 ml	0.252 ml	0.503 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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PCI-24781 (Abexinostat)