ABT-751 (E7010)

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

ABT-751 (E7010) Chemical Structure

CAS: 141430-65-1

规格 价格 库存 购买数量
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

ABT-751 (E7010)相关产品

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
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生物活性

产品描述 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。
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37oC/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4oC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Cmax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
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

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)

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

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)

mg/kg g μL

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,: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: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: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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