ABT-751 (E7010)

目錄號：S1165 Purity: 99.95%

ABT-751 (E7010)與β-tubulin的秋水仙素位點結(jié)合，抑制微管的聚合，不抑制MDR轉(zhuǎn)運的底物，且作用于抗Vincristine， Doxorubicin，和Cisplatin的細胞系有效。Phase 1/2。

ABT-751 (E7010) Chemical Structure

CAS: 141430-65-1

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1316.31	現(xiàn)貨
10mg	973.47	現(xiàn)貨
200mg	12858.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次： S116501 DMSO]74 mg/mL]false]Ethanol]12 mg/mL]false]Water]Insoluble]false 純度： 99.95%

99.95

ABT-751 (E7010)相關(guān)產(chǎn)品

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細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
HUVEC	Function assay	100-1000 nM	4 h	Induction of vascular disrupting activity in HUVEC assessed as VEGF-induced tube formation at 100 to 1000 nM after 4 hrs by microscopic analysis	24106982
P388 cell line	Function assay		72 h	Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in P388 cell line， IC50=0.19 μM	12383017
P388/4.0 r-M cell line	Function assay		72 h	Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in P388/4.0 r-M cell line, IC50=15 μM	12383017
HeLa cells	Cytotoxicity assay		48-72 h	Cytotoxicity against human HeLa cells after 48 to 72 hrs by WAT-1 assay, IC50=0.27 μM	21126027
MDR1 cells	Cytotoxicity assay		48-72 h	Cytotoxicity against human NCI-ADR-RES expressing MDR1 cells after 48 to 72 hrs by WAT-1 assay, IC50=0.29 μM	21126027
Jurkat cells	Function assay		24 h	Cell cycle arrest in human Jurkat cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis, IC50=0.16 μM	21126027
SW620 cells	Cytotoxicity assay		48-72 h	Cytotoxicity against human SW620 cells after 48 to 72 hrs by WAT-1 assay, IC50=0.19 μM	21126027
A2780 cells	Cytotoxicity assay		48-72 h	Cytotoxicity against human A2780 cells after 48 to 72 hrs by WAT-1 assay, IC50=0.17 μM	21126027
HT-29 cells	Proliferation assay		72 h	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50=0.21 μM	23202849
H460 cells	Cytotoxicity assay		72 h	Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.2177 μM	24106982
MKN45 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.166 μM	24106982
HT-29 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.3387 μM	24106982
human A549 cells	Cytotoxicity assay		48 h	Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50=1.31 μM	24835786
ACHN cells	Cytotoxicity assay		48 h	Cytotoxicity against human ACHN cells after 48 hrs by MTT assay, IC50=2.13 μM	24835786
MCF7 cells	Cytotoxicity assay		48 h	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=1.25 μM	24835786
HT-29 cells	Cytotoxicity assay		48 h	Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay, IC50=1.62 μM	24835786
A549 cells	Proliferation assay		24 h	Antiproliferative activity against human A549 cells assessed as growth inhibition after 24 hrs by SRB assay, GI50=1.31 μM	25468039
human MCF7 cells	Proliferation assay		24 h	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 24 hrs by SRB assay, GI50=1.25 μM	25468039
KB-S15 cells	Cytotoxicity assay		72 h	Cytotoxicity against human KB-S15 cells overexpressing P-gp170/MDR assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.206 μM	24106982
KB-7d cells	Cytotoxicity assay		72 h	Cytotoxicity against human KB-7d cells overexpressing MRP assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.205 μM	24106982
KB-VIN10 cells	Cytotoxicity assay		72 h	Cytotoxicity against human KB-VIN10 cells overexpressing P-gp170/MDR assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.227 μM	24106982
human PC3 cells	Cytotoxicity assay		48 h	Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay, GI50=0.62 μM	26241032
human AsPC1 cells	Cytotoxicity assay		48 h	Cytotoxicity against human AsPC1 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay, GI50=4.11 μM	26241032
human A549 cells	Cytotoxicity assay		48 h	Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay, GI50=5.33 μM	26241032
Hep3B cells	Cytotoxicity assay		48 h	Cytotoxicity against human Hep3B cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay, GI50=0.84 μM	26241032
KB cells	Cytotoxicity assay		72 h	Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.2513 μM	24106982
DU145 cells	Proliferation assay		24 h	Antiproliferative activity against human DU145 cells assessed as growth inhibition after 24 hrs by SRB assay, GI50=1.81 μM	25468039
DU145 cells	Cytotoxicity assay		48 h	Cytotoxicity against human DU145 cells after 48 hrs by MTT assay， GI50=1.81 μM	24835786
human SKBR3 cells	Growth inhibition assay		48 h	Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay, IC50=0.74 μM	22850214
HCT-15 cell	Proliferation assay			Antiproliferative activity against human colon carcinoma HCT-15 cell line(MDR(-)), IC50=0.34 μM	11425534
HCT116-C9 cell	Function assay			Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in HCT116-C9 cell line, IC50=0.9 μM	12383017
NCI-H460 cell	Proliferation assay			Antiproliferative activity against human lung carcinoma NCI-H460 cell line (MDR(+)), IC50=0.35 μM	11425534
human HL60 cells	Proliferation assay			Antiproliferative activity against human HL60 cells, IC50=0.34 μM	17276056
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

特性

ABT-751 是口服生物有效性的，與微管蛋白結(jié)合，抗有絲分裂的硫安類藥劑。

靶點

Microtubules ^[1]

體外研究(In Vitro)
體外研究活性	體外，ABT-751作用于神經(jīng)母細胞瘤時，IC50為0.6–2.6 μM，作用于其他實體瘤細胞系時，IC50為0.7–4.6 μM，且具有選擇毒性。而且, ABT-751也選擇性作用于動態(tài)微管, 可用于解釋濃度為ABT-751的IC90時的濃度時，α-微管陽性聚合小管持續(xù)乙?；?。^[1]
細胞實驗	細胞系	HOS, HTB-186 Daoy, TC-71, RD, SK-N-AS, SK-N-DZ, LD 和KCNR
	濃度	0 到100 μM
	孵育時間	72 小時
	方法	培養(yǎng)在含F(xiàn)BS的1640 RPMI培養(yǎng)基上的細胞接種在96孔組織培養(yǎng)板上，設(shè)計為最適合鋪滿單層細胞生長(HOS, HTB-186 Daoy細胞每孔5,000個;TC-71, RD, SK-N-AS, SK-N-DZ, LD細胞每孔10,000個; KCNR細胞每孔30,000個), 且具有一個自動化的，多通道的移液管系統(tǒng)。細胞在37^oC/5% CO₂下溫育24小時，然后用1.25% DMSO/H₂O（對照組）, VCR (0.1–1000 nM), ABT-751 (0.1 nM–100 μM)，和Combretastatin (0.1–1000 nM) 處理72 小時。細胞和三氯乙酸在4^oC下混合，終濃度為10%, 沖洗, 在室溫下烘干，用溶于1%乙酸的SRB染色，然后用Tris堿溶液染料。在540和 405 nm 雙波長下，在Bio-Tek EL 340 UV 讀數(shù)板上測定光密度。

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	ABT-751每天按100和75 mg/kg劑量單獨作用于Calu-6移植瘤模型，具有顯著抗癌活性，與Cisplatin聯(lián)用時, ABT-751進一步延遲腫瘤生長，這種作用存在劑量依賴性。ABT-751單獨作用于HT-29 結(jié)腸移植瘤模型，也具有顯著抗癌活性，與5-FU聯(lián)用時，也進一步延遲腫瘤生長，這種作用也存在劑量依賴性。^[2] ABT-751 作用于患淋巴癌的犬，具有劑量限制性毒性，伴隨著嘔吐，腹瀉，厭食，最大耐受劑量(MTD)為350 mg/m(2) PO q24h。而且, ABT-751按最大耐受劑量（MTD）350 mg/m(2) PO q24h 處理，平均AUC和C_max分別為5.55 μg-hour/mL和0.9 μg/mL。^[3]
動物實驗	Animal Models	注射Calu-6 NSCLC, HT-29 結(jié)腸, 和 HCT-116細胞的無胸腺小鼠
	Dosages	75 或100 mg/kg/day
	Administration	口服處理

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)
NCT00436852	Completed	Disseminated Neuroblastoma\|Recurrent Neuroblastoma	Children''s Oncology Group\|National Cancer Institute (NCI)	January 2007	Phase 2
NCT00735878	Terminated	Non Small Cell Lung Cancer\|Lung Cancer	Konstantin Dragnev\|Abbott\|Dartmouth-Hitchcock Medical Center	September 2004	Phase 1\|Phase 2

參考文獻
[1] Meany HJ, et al. Pediatr Blood Cancer. 2010, 54(1), 47-54. [2] Jorgensen TJ, et al. Cancer Chemother Pharmacol. 2007, 59(6), 725-732. [3] Silver M, et al. J Vet Intern Med. 2012, 26(2), 349-354.

參考文獻

[1] Meany HJ, et al. Pediatr Blood Cancer. 2010, 54(1), 47-54.
[2] Jorgensen TJ, et al. Cancer Chemother Pharmacol. 2007, 59(6), 725-732.
[3] Silver M, et al. J Vet Intern Med. 2012, 26(2), 349-354.

化學(xué)信息&溶解度

分子量	371.41	分子式	C₁₈H₁₇N₃O₄S
CAS號	141430-65-1	SDF	Download ABT-751 (E7010) SDF
Smiles	COC1=CC=C(C=C1)S(=O)(=O)NC2=C(N=CC=C2)NC3=CC=C(C=C3)O
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(fù)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(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 74 mg/mL ( (199.24 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 12 mg/mL (32.3 mM)

Water : 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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