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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
ABT-751
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
141430-65-1
- 规格：
25mg/5mg/50mg/10mg
| 规格： | 25mg | 产品价格： | ￥1490.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥490.0 |
| 规格： | 50mg | 产品价格： | ￥2190.0 |
| 规格： | 10mg | 产品价格： | ￥740.0 |
是新型的生物相容性的微管蛋白结合剂和抗有丝分裂磺胺类化合物。
| 基本信息 | |
| CAS | No.141430-65-1 |
| 英文名称 | ABT-751 |
| 别名 | E7010 |
| 分子式 | C18H17N3O4S |
| 分子量 | 371.41 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC | EINECS 256-495-9 |
| MDL | MFCD00910291 |
| SMILES | COC1=CC=C(C=C1)S(=O)(NC2=C(N=CC=C2)NC3=CC=C(C=C3)O)=O |
| 靶点 | Microtubule/Tubulin |
| 通路 | Cytoskeleton |
| 背景说明 | ABT-751/E-7010是新型的生物相容性的微管蛋白结合剂和抗有丝分裂磺胺类化合物。 |
| 生物活性 | ABT-751 (Abbott Laboratories， Abbott Park， IL) is an orally bioavailable sulfonamide that binds to the colchicine binding site on β-tubulin and inhibits the polymerization of microtubules. ABT-751 had antitumor activity in a panel of 30 tumor cell lines in vitro including cell lines resistant to Vinca alkaloids and taxanes due to P-glycoprotein overexpression. ABT-751 is a novel orally available antimitotic agent that targets microtubule polymerization.[1-2] |
| 细胞实验 | The maximum tolerated dose of ABT-751 was 350 mg/m(2)PO q24h. Dose-limiting toxicities included vomiting and diarrhea，which resolved with a schedule adjustment to 350 mg/m(2)PO q48h. ABT-751 was consistently detected in lymphoma tissue samples from dogs treated at or above the maximum tolerated dose. In the cohort expansion，objective responses were seen in 3/15(20%)dogs with a response duration ranging from 21 to 111 days. Decreases in circulating endothelial cells were seen in 10 dogs at day 7(2 responding dogs and 8 nonresponding dogs).[2] |
| 动物实验 | Dogs(n = 11)were enrolled in a rapid dose escalation study to define the maximum tolerated dose. Upon definition of a maximally tolerated dose，a cohort expansion of 19 dogs allowed verification of long-term tolerability and assessment of activity. Study endpoints in the cohort expansion included chronic tolerability，response rate，response duration，and time to progression. Additional endpoints included serum pharmacokinetics，lymph node drug concentrations，and changes in circulating endothelial cells.[2] |
| 数据来源文献 | [1]. Elizabeth Fox et al. A Phase I Study of ABT-751， an Orally Bioavailable Tubulin Inhibitor， Administered Daily for 21 Days Every 28 Days in Pediatric Patients with Solid Tumors Clin Cancer Res February 15， 2008 14; 1111 [2]. Silver M， Rusk A， Phillips B， Beck E， Jankowski M， Philibert J， Hahn K， Hershey E， McKeegan E， Bauch J， Krivoshik A， Khanna C.，Evaluation of the oral antimitotic agent (ABT-751) in dogs with lymphoma.，J Vet Intern Med. 2012 Mar-Apr;26(2):349-54. doi: 10.1 |
| 单位 | 瓶 |
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