PHA-665752
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.
PHA-665752是ATP竞争性、有效的、特定的c-Met受体酪氨酸激酶抑制剂，Ki值4 nM，IC50值9 nM。PHA-665752对c-Met的选择性是丝氨酸/苏氨酸激酶和酪氨酸激酶的50多倍[1]。
已证实PHA-665752能抑制肝细胞生长因子(HGF)和c-Met调节的胰脏癌细胞BxPC-3、胃癌细胞GTL-16和肺癌细胞NCI-H441的细胞增殖、运动性、入侵和形态学。此外，PHA-665752抑制HGF引起的c-Met下游介质的磷酸化[1]。
在体内，PHA-665752在移植了无胸腺的小鼠S114和GTL-16中抑制c-Met磷酸化及肿瘤生长[1]。
参考文献：
[1]. Christensen JG1, Schreck R, Burrows J, Kuruganti P, Chan E, Le P, Chen J, Wang X, Ruslim L, Blake R, Lipson KE, Ramphal J, Do S, Cui JJ,Cherrington JM, Mendel DB. A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. Cancer Res. 2003 Nov 1;63(21):7345-55.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 641.61 |
| Cas No. | 477575-56-7 |
| Formula | C32H34Cl2N4O4S |
| Solubility | insoluble in H2O; ≥3.1 mg/mL in EtOH with ultrasonic; ≥32.1 mg/mL in DMSO |
| Chemical Name | (3Z)-5-[(2,6-dichlorophenyl)methylsulfonyl]-3-[[3,5-dimethyl-4-[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]-1H-pyrrol-2-yl]methylidene]-1H-indol-2-one |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(NC(=C1C(=O)N2CCCC2CN3CCCC3)C)C=C4C5=C(C=CC(=C5)S(=O)(=O)CC6=C(C=CC=C6Cl)Cl)NC4=O |
| 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。 |
| 描述 | PHA-665752是c-Met的ATP竞争性、有效的、选择性抑制剂（IC50值9 nM），对c-Met的选择性是RTKs或STKs的50多倍。 | |||||
| 靶点 | c-Met | |||||
| IC50 | 9 nM | |||||
化学结构
相关生物数据
相关生物数据
相关生物数据
