RMC-4550
规格
| Cas Number | 2172651-73-7 |
| 规格或纯度 | ≥99% |
| 纯度 | ≥99% |
| 包装 | 1mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 87 mg/mL (198.92 mM); Ethanol: 15 mg/mL (34.29 mM); Water: Insoluble; |
| 简短描述 | 磷酸酶抑制剂 |
| 英文简短描述 | phosphatase Inhibitors |
| 过滤标签 | Phosphatase,SHP2,Protein Tyrosine Kinase/RTK,Metabolic Enzyme/Protease |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | RMC-4550 是一种强效的 SHP-2 抑制剂，其 IC50 值为 1.55 nM，对 468 种激酶、15 种磷酸酶的催化结构域以及包括 GPCR、转运体和离子通道在内的其他细胞靶标无明显活性。 |
| 英文描述 |
Information RMC-4550 RMC-4550 is a potent SHP-2 inhibitor with an IC50 of 1.55 nM and it has no significant activity vs. 468 kinases, the catalytic domain of 15 phosphatases and other cellular targets including GPCRs, transporters and ion channels. Targets SHP-2 (Cell-free assay) 1.55 nM In vitro RMC-4550 inhibits purified, activated full length human SHP2 with an IC50 of 1.55 nM, and has cellular IC50 of 39 nM in PC9 cells with a pERK readout. RMC-4550 has no detectable inhibitory activity up to 10 µM against the catalytic domain of SHP2, a panel of 14 additional protein phosphatases, and a panel of 468 protein kinases. RMC-4550 exhibits low to moderate cross species in vitro intrinsic clearance (3.6-24 µL/min/million cells) in hepatocytes, a high passive permeability (458 nm/s) and efflux ratio of 1. In vivo RMC-4550 has moderate to high bioavailability and has a half-life amenable for once daily oral administration. In the EGFR-driven KYSE-520 human esophageal cancer xenograft model, RMC-4550 has a dose dependent efficacy consistent with target modulation, assessed by phospho-ERK inhibition in tumors. RMC-4550 is well tolerated at doses that achieved maximal and sustained efficacy in this model. Cell Research(from reference) Cell lines：HEK-293 cells Incubation Time：1 h |