Amuvatinib (MP-470, HPK 56)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Amuvatinib（也称MP-470或HPK 56），是一种合成的硫代酰胺，是一种新型有效的酪氨酸激酶抑制剂，对包括突变KIT、血小板衍生生长因子受体alpha（PDGFRα）和DNA修复在内的多个靶点具有体外和体内活性。机理上说，amuvatinib可通过占据ATP结合结构域，抑制酪氨酸激酶受体KIT（IC50 < 0.1 μM），通过抑制同源重组蛋白Rad51扰乱DNA修复，并能与双链DNA损伤剂产生协同效应。近期研究表明，amuvatinib对多个人类肿瘤细胞系具有抗肿瘤活性，特别是在GIST-48人类细胞系中，可以强力抑制增殖（IC50 = 0.20 μM）。
参考文献：
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
Gavin Choy, Rajashree Joshi-Hangal, Aram Oganesian, Gil Fine, Scott Rasmussen, Joanne Collier, James Kissling, Amarpal Sahai, Mohammad Azab and Sanjeev Redkar. Saftety, tolerability, and pharmacokinetics of amuvatinib from three phase 1 clinical studies in healthy volunteers. Cancer Chemother Pharmacol (2012) 70: 183-190
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 447.51 |
| Cas No. | 850879-09-3 |
| Formula | C23H21N5O3S |
| Synonyms | MP470,MP 470,HPK56 |
| Solubility | ≥22.4 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | N-(1,3-benzodioxol-5-ylmethyl)-4-([1]benzofuro[3,2-d]pyrimidin-4-yl)piperazine-1-carbothioamide |
| SDF | Download SDF |
| Canonical SMILES | C1CN(CCN1C2=NC=NC3=C2OC4=CC=CC=C43)C(=S)NCC5=CC6=C(C=C5)OCO6 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | Amuvatinib（MP-470）是一种有效的c-Kit、PDGFRα和Flt3多靶点抑制剂，IC50值分别为10 nM、40 nM和81 nM。 | |||||
| 靶点 | c-KitD816H | PDGFRαV561D | Flt3D835Y | |||
| IC50 | 10 nM | 40 nM | 81 nM | |||
化学结构
相关生物数据
相关生物数据
