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PF-4708671

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Chemical Structure| 1255517-76-0 同义名 : PF-04708671
CAS号 : 1255517-76-0
货号 : A130606
分子式 : C19H21F3N6
纯度 : 99%+
分子量 : 390.406
MDL号 : MFCD18086922
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(89.65 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
描述 PF-4708671 is the first reported highly specific p70 S6K1 (p70 ribosomal S6 kinase) inhibitor with Ki value of 20nM and IC50 value of 160nM. PF-4708671 at concentration of 3μM and 10μM prevented the S6K1-mediated phosphorylation of S6 protein (S235/236, S240/S244) in response to IGF-1, while having no effect upon the PMA-induced phosphorylation of substrates of the highly related RSK (p90 ribosomal S6 kinase) and MSK (mitogen- and stress-activated kinase) kinases. Also, it dose-dependently induced phosphorylation of S6K1 at Thr229 and Thr389 at concentration ranging in 3-10μM in HEK-293 cells after serum starvation for 16h, dependent upon mTORC1[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
22RV1 Growth Inhibition Assay IC50=47.9015 μM SANGER
23132-87 Growth Inhibition Assay IC50=44.2978 μM SANGER
639-V Growth Inhibition Assay IC50=84.6129 μM SANGER
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.81mL

2.56mL

1.28mL

25.61mL

5.12mL

2.56mL
参考文献

[1]Pearce LR, Alton GR, et al. Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem J. 2010 Oct 15;431(2):245-55.

[2]Pearce LR, Alton GR, Richter DT, Kath JC, Lingardo L, Chapman J, Hwang C, Alessi DR. Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem J. 2010 Oct 15;431(2):245-55. doi: 10.1042/BJ20101024. PMID: 20704563.