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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Protein Phosphatase/PTP-RMC-4550
RMC-4550

Chemical Structure : RMC-4550

CAS No.: 2172651-73-7

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RMC-4550 (RMC4550)

货号: PC-35116Not For Human Use, Lab Use Only.

RMC-4550 (RMC4550) is a potent, selective, allosteric inhibitor of SHP2 with IC50 of 0.58 nM (full-length SHP2 enzyme), suppresses pERK signaling in Calu-1 cells with IC50 of 7 nM.

规格 价格 库存 数量
5 mg ￥1380 In stock
10 mg ￥2180 In stock
25 mg ￥3580 In stock
50 mg ￥5580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: 98.12% (HPLC) Select Batch:

生物&药学活性

RMC-4550 (RMC4550) is a potent, selective, allosteric inhibitor of SHP2 with IC50 of 0.58 nM (full-length SHP2 enzyme), suppresses pERK signaling in Calu-1 cells with IC50 of 7 nM.
RMC-4550 shows no activity against the SHP2 catalytic domain up to 10 uM, RMC-4550 is highly selective for full-length SHP2 across panels comprising 15 other phosphatases, 468 kinases, and 44 cellular targets.
Cancer cell lines bearing missense mutations in KRAS at G12, but neither G13 nor Q61, exhibit sensitivity to RMC-4550 (IC50<2 uM), suppresses growth and RAS/MAPK signaling in cancer cell lines with Class 3 BRAF mutations.
RMC-4550 inhibits tumor growth and RAS/MAPK signaling in xenograft models of KRASG12C-driven cancer.

物理化学性质&存储条件

分子量 437.365
分子式 C21H26Cl2N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-Pyrazinemethanol, 3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]dec-8-yl]-6-(2,3-dichlorophenyl)-5-methyl-

参考文献

1. Robert J. Nichols, et al. Efficacy of SHP2 phosphatase inhibition in cancers with nucleotide-cycling oncogenic RAS, RAS-GTP dependent oncogenic BRAF and NF1 loss. http://dx.doi.org/10.1101/188730.

2. Nichols RJ, et al. Nat Cell Biol. 2018 Sep;20(9):1064-1073.

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