ABT-751 (E7010)

目录号：S1165 Purity: 99.95%

ABT-751 (E7010)与β-tubulin的秋水仙素位点结合，抑制微管的聚合，不抑制MDR转运的底物，且作用于抗Vincristine， Doxorubicin，和Cisplatin的细胞系有效。Phase 1/2。

ABT-751 (E7010) Chemical Structure

CAS: 141430-65-1

规格	价格	库存
10mM (1mL in DMSO)	1316.31	现货
10mg	973.47	现货
200mg	12858.3	现货
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产品质控

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

99.95

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细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
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
点击查看更多细胞系数据

生物活性

产品描述

特性

ABT-751 是口服生物有效性的，与微管蛋白结合，抗有丝分裂的硫安类药剂。

靶点

Microtubules ^[1]

体外研究(In Vitro)
体外研究活性	体外，ABT-751作用于神经母细胞瘤时，IC50为0.6–2.6 μM，作用于其他实体瘤细胞系时，IC50为0.7–4.6 μM，且具有选择毒性。而且, ABT-751也选择性作用于动态微管, 可用于解释浓度为ABT-751的IC90时的浓度时，α-微管阳性聚合小管持续乙酰化。^[1]
细胞实验	细胞系	HOS, HTB-186 Daoy, TC-71, RD, SK-N-AS, SK-N-DZ, LD 和KCNR
	浓度	0 到100 μM
	孵育时间	72 小时
	方法	培养在含FBS的1640 RPMI培养基上的细胞接种在96孔组织培养板上，设计为最适合铺满单层细胞生长(HOS, HTB-186 Daoy细胞每孔5,000个;TC-71, RD, SK-N-AS, SK-N-DZ, LD细胞每孔10,000个; KCNR细胞每孔30,000个), 且具有一个自动化的，多通道的移液管系统。细胞在37^oC/5% CO₂下温育24小时，然后用1.25% DMSO/H₂O（对照组）, VCR (0.1–1000 nM), ABT-751 (0.1 nM–100 μM)，和Combretastatin (0.1–1000 nM) 处理72 小时。细胞和三氯乙酸在4^oC下混合，终浓度为10%, 冲洗, 在室温下烘干，用溶于1%乙酸的SRB染色，然后用Tris碱溶液染料。在540和 405 nm 双波长下，在Bio-Tek EL 340 UV 读数板上测定光密度。

体内研究(In Vivo)
体内研究活性	ABT-751每天按100和75 mg/kg剂量单独作用于Calu-6移植瘤模型，具有显著抗癌活性，与Cisplatin联用时, ABT-751进一步延迟肿瘤生长，这种作用存在剂量依赖性。ABT-751单独作用于HT-29 结肠移植瘤模型，也具有显著抗癌活性，与5-FU联用时，也进一步延迟肿瘤生长，这种作用也存在剂量依赖性。^[2] ABT-751 作用于患淋巴癌的犬，具有剂量限制性毒性，伴随着呕吐，腹泻，厌食，最大耐受剂量(MTD)为350 mg/m(2) PO q24h。而且, ABT-751按最大耐受剂量（MTD）350 mg/m(2) PO q24h 处理，平均AUC和C_max分别为5.55 μg-hour/mL和0.9 μg/mL。^[3]
动物实验	Animal Models	注射Calu-6 NSCLC, HT-29 结肠, 和 HCT-116细胞的无胸腺小鼠
	Dosages	75 或100 mg/kg/day
	Administration	口服处理

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (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

参考文献
[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.

参考文献

化学信息&溶解度

分子量	371.41	分子式	C₁₈H₁₇N₃O₄S
CAS号	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
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 74 mg/mL ( (199.24 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 12 mg/mL (32.3 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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