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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ribosomal S6 Kinase (RSK)-M2698
M2698

Chemical Structure : M2698

CAS No.: 1379545-95-5

M2698 (MSC-2363318A, MSC2363318A, M 2698)

货号: PC-60433Not For Human Use, Lab Use Only.

M2698 (MSC2363318A) is a potent, selective, ATP-competitive, orally bioavailable and brain penetrant dual inhibitor of p70S6K and Akt1/3 with IC50 of 1 nM and 17 nM, respectively.

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10 mg ¥2880 In stock
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50 mg ¥7880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

M2698 (MSC2363318A) is a potent, selective, ATP-competitive, orally bioavailable and brain penetrant dual inhibitor of p70S6K and Akt1/3 with IC50 of 1 nM and 17 nM, respectively.
M2698 displays relative selectivity against a panel of 264 kinases (only 6 kinases within 10-fold IC50 of p70S6K).
M2698 inhibits the phosphorylation of p70S6K1 and Akt substrates, S6 (IC50=11 nM) and GSK3β (IC50=17 nM) in MDA-MB-468 cells, shows proliferation inhibition of 9 breast cancer cell lines (IC50<2 uM).
M2698  inhibits growth of human breast cancer xenografted tumors in mice.

物理化学性质&存储条件

分子量 449.862
分子式 C21H19ClF3N5O
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

(S)-4-((2-(azetidin-1-yl)-1-(4-chloro-3-(trifluoromethyl)phenyl)ethyl)amino)quinazoline-8-carboxamide

参考文献

1. Machl A, et al. Am J Cancer Res. 2016 Mar 15;6(4):806-18.

2. Previs RA, et al. J Natl Cancer Inst. 2017 Jul 1;109(7).

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