| CAS NO: | 850879-09-3 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 850879-09-3 |
| 别名 | N-(1,3-苯并二氧戊环-5-基甲基)-4-苯并呋喃并[3,2-D]嘧啶-4-基-1-哌嗪硫代甲酰胺,MP470,MP 470,HPK56 |
| 化学名 | N-(1,3-benzodioxol-5-ylmethyl)-4-([1]benzofuro[3,2-d]pyrimidin-4-yl)piperazine-1-carbothioamide |
| Canonical SMILES | C1CN(CCN1C2=NC=NC3=C2OC4=CC=CC=C43)C(=S)NCC5=CC6=C(C=C5)OCO6 |
| 分子式 | C23H21N5O3S |
| 分子量 | 447.51 |
| 溶解度 | ≥ 22.4 mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Amuvatinib (also known as MP-470 or HPK 56), a synthetic carbothioamide, is a novel and potent tyrosine kinase inhibitor, which exertsin vitroandin vivoactivities against multiple targets including mutant KIT, platelet-derived growth factor receptor alpha (PDGFRα) and DNA repair. Μechanisticly, amuvatinib inhibits tyrosine kinase receptor KIT through occupying its ATP binding domain (IC50< 0.1 μM) and disrupts DNA repair through suppression of homologous recombination protein Rad51 as well as synergistic effects in combination with double stranded DNA damaging agents. Recent studies have shown that amuvatinib exhibits antitumor activity against human cancer cell lines, especially GIST-48 human cell line, in which it strongly inhibits proliferation (IC50= 0.20 μM). Reference [1].Raoul Tibes, Gil Fine, Gavin Choy, Sanjeev Redkar, Pietro Taverna, Aram Oganesian, Amarpao Sahai, Mohammad Azab and Anthony W. Tolcher. A phase I, first-in-human dose-escalation study of amuvatinib, a multi-targeted tyrosine kinase inhibitor, in patients with advanced solid tumors. Cancer Chemother Pharmacol (2013) 71: 463-471 |
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