Abexinostat (PCI-24781)

別名: CRA-024781 中文名稱：艾貝司他

目錄號：S1090 Purity: 98.89%

Abexinostat (PCI-24781, CRA-024781) 是一種新型的pan-HDAC抑制劑，靶向作用于HDAC1，K_i為7 nM，對HDACs 2， 3， 6，和10有適中的抑制性，但比作用于HDAC8選擇性強40倍。Phase 1/2。

Abexinostat (PCI-24781) Chemical Structure

CAS: 783355-60-2

規(guī)格	價格	庫存
10mM (1mL in DMSO)	2217.61	現(xiàn)貨
5mg	1406.39	現(xiàn)貨
10mg	2628.91	現(xiàn)貨
50mg	7938.64	現(xiàn)貨
1g	31941	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 98.89%

98.89

Abexinostat (PCI-24781)相關(guān)產(chǎn)品

相關(guān)靶點	HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2	點擊展開
相關(guān)產(chǎn)品	Entinostat (MS-275) TSA (Trichostatin A) Mocetinostat (MGCD0103) RGFP966 Tubastatin A Ricolinostat (ACY-1215) Quisinostat (JNJ-26481585) 2HCl MC1568 Tubastatin A HCl PCI-34051 Tacedinaline (CI994) LMK-235 Fimepinostat (CUDC-907) Tubacin Givinostat (ITF2357) TMP269 AR-42 Sodium butyrate Pracinostat (SB939) Santacruzamate A (CAY10683) (-)-Parthenolide CUDC-101 Dacinostat (LAQ824) CAY10603 RG2833 (RGFP109) Tasquinimod Tucidinostat (Chidamide) TMP195 Nexturastat A Droxinostat Domatinostat (4SC-202) Scriptaid 4-PBA (4-Phenylbutyric acid) M344 Resminostat Citarinostat (ACY-241) BG45 WT161 ACY-738 HPOB ITSA-1 (ITSA1) Tubastatin A TFA TC-H 106 SIS17 ACY-775 BML-210 (CAY10433) TH34 Raddeanin A	點擊展開
相關(guān)化合物庫	激酶抑制劑庫血管生成相關(guān)化合物庫 TGF-beta/Smad信號通路庫細胞骨架信號通路化合物庫抗心血管疾病化合物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	孵育時間	活性描述	文獻信息
HeLa	Function assay	2 hrs	Inhibition of dye-labeled tracer binding to HDAC10 (unknown origin) transfected in human HeLa cells measured after 2 hrs by nano-luciferase reporter gene-based BRET assay, IC50=0.007943μM	30964290
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
U-2 OS	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
U-2 OS	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Rh18	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Rh30	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點

HDAC1 ^[1] (Cell-free assay)	HDAC3/SMRT ^[1]	HDAC6 ^[1]	HDAC2 ^[1] (Cell-free assay)	HDAC10 ^[1]	點擊更多
7 nM(Ki)	8.2 nM(Ki)	17 nM(Ki)	19 nM(Ki)	24 nM	點擊更多

體外研究(In Vitro)
體外研究活性	PCI-24781針對于多種腫瘤細胞系具有有效的抗腫瘤活性，GI50分布于0.15 μM 到3.09 μM之間。PCI-24781也抑制HUVEC 內(nèi)皮細胞的增值，GI50為0.43 μM。PCI-24781處理導致HCT116 和 DLD-1細胞系中組蛋白乙?；臀⒐艿鞍滓阴；膭┝恳蕾囆苑e累，同時誘導p21表達，PARP的剪切以及γH2AX的累積^[1]。PCI-24781抑制HDACs酶活導致HR 相關(guān)基因的轉(zhuǎn)錄水平出現(xiàn)明顯下降，其中包括RAD51。與抑制HR 一致，在CHO細胞中，PCI-24781處理后導致I-SceI誘導染色質(zhì)斷裂引起的同源定向修復能力下降^[2]。PCI-24781誘發(fā)S 期缺失，G2期細胞周期停滯以及軟組織（STS）細胞的凋亡。PCI-24781誘導STS細胞中Rad51 的轉(zhuǎn)錄抑制很有可能是通過增強E2F1在Rad51近端啟動子區(qū)域的結(jié)合^[3]。PCI-24781也誘導Hodgkin淋巴瘤和非霍奇金淋巴瘤中蛋白酶和活性氧依賴的NF-κB信號通路介導的細胞凋亡過程^[4]。
激酶實驗	HDAC 酶活鑒定
激酶實驗	運用連續(xù)胰蛋白酶耦合分析法檢測HDAC酶活。將100μL反應體系置于96孔板中分析抑制劑表征。將HDAC 酶添加到50 mM HEPES, 100 mM KCl, 0.001% Tween 20, 5% DMSO (pH 7.4) 以及補充了牛血清蛋白 (BSA)的反應體系中，與不同濃度的PCI-24781混合均勻，孵育15分鐘。每種HDAC同工酶使用的BSA濃度不一樣，分別是0% (HDAC1)，0.01% (HDAC2, 3, 8, 10)和0.05% (HDAC6)。胰蛋白酶的終濃度是50 nM，acetyl-Gly-Ala-(N-acetyl-Lys)-AMC的終濃度是25μM(HDAC1,HDAC3,HDAC6),50μM (HDAC2,HDAC10)和100 μM (HDAC8)，起始反應。設置八個復孔的陰性對照中不加入PCI-24781。使用酶標儀檢測反應。經(jīng)過30分鐘的延遲時間，通過355納米的激發(fā)波和460納米吸收波得到熒光值。檢測反應速率是測定增強熒光所需的反應時間。使用程序BatchK_i可以得到抑制常數(shù)K _i (app)
細胞實驗	細胞系	HCT116, HCT-15, BT-549, NCI-H226, CWR-22RV1, MCF-7, NCI-PC3, DLD-1, SKOV-3和 OVCAR-3細胞
	濃度	0–10 μM，溶于 DMSO
	孵育時間	48, 72, 96和120 小時
	方法	運用一種微量藍色熒光的細胞增殖試驗檢測PCI-24781處理后細胞增殖，細胞至少培養(yǎng)兩倍增。細胞接種于96孔板，PCI-24781設置9個從0.0015 μM 到10 μM半對數(shù)不等間隔的濃度梯度，每一梯度設計三個復孔。DMSO終濃度每孔0.15%。設定抑制細胞增殖GI50在達到50% 到 95%之間為置信區(qū)間，運用四參數(shù)方程，利用非線性回歸曲線計算PCI-24781的有效濃度。

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	PCI-24781按200 mg/kg 劑量作用于移植小鼠，隔一天一次,明顯抑制HCT116 和 DLD-1腫瘤細胞生長，抑制效果分別是69%和59%。PCI-24781按20 mg/kg, 40 mg/kg, 80 mg/kg和160 mg/kg劑量每星期連續(xù)四天給藥處理，然后三天不給藥處理((一天一次，每周四天))作用于HCT116移植小鼠模型，抑制效果分別是48%, 57%, 82.2%, 和80.0%^[1]。
動物實驗	Animal Models	攜帶HCT116 和DLD-1移植瘤細胞的BALB/c nu/nu 雌小鼠
	Dosages	~200 mg/kg
	Administration	每隔一天一次或者每星期連續(xù)四天，停滯三天。

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05698524	Recruiting	Recurrent High Grade Glioma\|Anaplastic Astrocytoma\|Anaplastic Oligodendroglioma\|Glioblastoma\|Gliosarcoma	University of Nebraska\|Xynomic Pharmaceuticals Inc.	June 26 2023	Phase 1
NCT03934567	Recruiting	Lymphoma Follicular	Xynomic Pharmaceuticals Inc.	April 22 2020	Phase 2
NCT03939182	Active not recruiting	Diffuse Large B-cell Lymphoma\|Mantle Cell Lymphoma	Memorial Sloan Kettering Cancer Center\|Janssen Scientific Affairs LLC\|Xynomic Pharmaceuticals Inc.	May 29 2019	Phase 1
NCT03600441	Active not recruiting	Follicular Lymphoma	Xynomic Pharmaceuticals Inc.	August 27 2018	Phase 2
NCT01543763	Active not recruiting	Metastatic Solid Tumors	Pamela Munster\|Pharmacyclics LLC.\|Novartis\|Xynomic Pharmaceuticals Inc.\|GlaxoSmithKline Research and Education Foundation for Cardiovascular Disease\|University of California San Francisco	June 25 2012	Phase 1

參考文獻
[1] Buggy JJ, et al. Mol Cancer Ther, 2006, 5(5), 1309-1317. [2] Adimoolam S, et al. Proc Natl Acad Sci U S A, 2007, 104(49), 19482-19487. [3] Lopez G, et al. Clin Cancer Res, 2009, 15(10), 3472-3483. [4] Bhalla S, et al. Clin Cancer Res, 2009, 15(10), 3354-3365. + 展開

參考文獻

[1] Buggy JJ, et al. Mol Cancer Ther, 2006, 5(5), 1309-1317.
[2] Adimoolam S, et al. Proc Natl Acad Sci U S A, 2007, 104(49), 19482-19487.
[3] Lopez G, et al. Clin Cancer Res, 2009, 15(10), 3472-3483.

[4] Bhalla S, et al. Clin Cancer Res, 2009, 15(10), 3354-3365.

+ 展開

化學信息&溶解度

分子量	397.42	分子式	C₂₁H₂₃N₃O₅
CAS號	783355-60-2	SDF	Download Abexinostat (PCI-24781) SDF
Smiles	CN(C)CC1=C(OC2=CC=CC=C21)C(=O)NCCOC3=CC=C(C=C3)C(=O)NO
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

5%TFA : 3 mg/mL (7.54 mM)

DMSO : Insoluble ( ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

DMSO : 5 mg/mL ( (12.58 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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