- 目录号: HY-15773 纯度: 99.85%
- COA 产品使用指南
FAQs
PF-4708671 是一种有效的细胞渗透性 S6K1 抑制剂,Ki 为 20 nM,IC50 为 160 nM。
MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务
PF-4708671 Chemical Structure
CAS No. : 1255517-76-0
1.客户无需承担相应的运输费用。
2.同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内
可免费申领三个不同产品的试用装。
3.试用装只面向终端客户。
规格 | 价格 | 是否有货 | 数量 |
---|---|---|---|
10mM*1 mL in DMSO | ¥649 | In-stock | |
1 mg | ¥184 | In-stock | |
5 mg | ¥368 | In-stock | |
10 mg | ¥590 | In-stock | |
25 mg | ¥1150 | In-stock | |
50 mg | ¥1955 | In-stock | |
100 mg | ¥3300 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
or 大包装询价
* Please select Quantity before adding items.
Customer Review
MCE 顾客使用本产品发表的 17 篇科研文献
- •Cancer Discov. 2022 Jun 8;candisc.1672.2021. [Abstract]
- •J Infect.2019 Sep;79(3):262-276. [Abstract]
- •Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. [Abstract]
- •Cell Rep. 2021 Jun 22;35(12):109277. [Abstract]
- •Free Radic Biol Med. 2022 Dec 7;194:184-198. [Abstract]
- •Pestic Biochem Phys. 2023 Apr.
- •Food Biosci. April 2022, 101571.
- •Front Neurol. 2018 Apr 9;9:208. [Abstract]
- •J Proteomics. 2016 Feb 2;136:13-24. [Abstract]
- •Research Square Preprint. 2024 Jan 31.
- •bioRxiv. 2023 Feb 15.
- •Oxid Med Cell Longev. 25 Aug 2022.
- •Research Square Preprint. 2021 Sep.
- •Patent. US20200376102A1.
- •Patent. US20200376146A1.
- •bioRxiv. 2020 Apr.
- •Harvard Medical School LINCS LIBRARY
WB
-
PF-4708671 purchased from MCE. Usage Cited in: J Proteomics. 2016 Feb 2;136:13-24. [Abstract]
- mTORC1 regulates KPNA2 transcription but not S6K1- and 4E-BP1-dependent translation. KPNA2 abundances in response to S6K1 inhibition are detected by Western blot analysis in WT and TSC2−/− MEFs.
PF-4708671 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Immunology/Inflammation Compound Library
- Kinase Inhibitor Library
- MAPK Compound Library
- Anti-Cancer Compound Library
- Autophagy Compound Library
- Reprogramming Compound Library
- Oxygen Sensing Compound Library
- Glutamine Metabolism Compound Library
- Anti-Cancer Metabolism Compound Library
- Anti-Obesity Compound Library
- Chemokine Compound Library
- Highly Selective Inhibitors Library
- Highly Selective Activators Library
- Cell Death Library
- Serine/Threonine Kinase Inhibitor Library
- Multi-Target Compound Library
- Bioactive Compound Library Max
查看 Ribosomal S6 Kinase (RSK) 亚型特异性产品:
查看所有亚型
p70S6K RSK1 RSK2 RSK3 RSK4
生物活性
实验参考方法
纯度 & 产品资料
参考文献
生物活性 | PF-4708671 is a potent cell-permeable S6K1 inhibitor with a Ki of 20 nM and IC50 of 160 nM. | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
IC50 & Target[1] |
| ||||||||||||
体外研究 (In Vitro) | PF-4708671 inhibits the activity of full-length S6K1 in vitro with a Ki of 20 nM, and S6K1 isolated from IGF1-stimulated HEK293 cells with an IC50 of 0.16 μM, and only inhibits very weakly the closely related S6K2 isoform (IC50 of 65 μM). PF-4708671 inhibits RSK1 (IC50 of 4.7 μM) and RSK2 (IC50 of 9.2 μM) over 20-fold less potently than S6K1. PF4708671 inhibits MSK1 (IC50 of 0.95 μM) 4-fold more weakly than S6K1[1]. HCT116 cells are treated with (i) vehicle (DMSO), (ii) OSI-906 (5 μM), (iii) PF-4708671 (10 μM), and (iv) OSI-906 (5 μM)+PF-4708671 (10 μM) for various amounts of time. HCT116 cells treated with OSI-906 alone (closed square) or PF4708671 alone (open circle) slightly inhibit cell growth. In contrast, proliferation in HCT116 cells is significantly inhibited after a 2-day treatment with the combination of OSI-906 and PF-4708671 (closed circle). A similar result is also observed when SW480 cells are treated with the combination of OSI-906 and PF-4708671. Colony formation also significantly reduces in OSI-906+PF-4708671-treated cells comparing with vehicle, OSI-906 alone, or PF-4708671 alone treated HCT116 or SW480 cells[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||
体内研究 (In Vivo) | The tumor growth rate in mice treated with the combination of OSI-906+PF-4708671 is significantly slower than that of OSI-906 alone (P=0.0189) or PF4708671 alone (P=0.0165) treated mice. The average tumor volume in the OSI-906+PF-4708671-treated mice is approximately 50% of that in mice treated with OSI-906 (P=0.0056) or PF-4708671 alone (P<0.001) at the end of a 15-day treatment[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||
分子量 | 390.41 | ||||||||||||
Formula | C19H21F3N6 | ||||||||||||
CAS 号 | 1255517-76-0 | ||||||||||||
性状 | 固体 | ||||||||||||
颜色 | White to off-white | ||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||
储存方式 |
| ||||||||||||
溶解性数据 | 细胞实验: DMSO 中的溶解度 : 33.33 mg/mL (85.37 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO) 配制储备液
查看完整储备液配制表 * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 动物实验: 请根据您的 实验动物和给药方式 选择适当的溶解方案。 以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
动物溶解方案计算器 请输入动物实验的基本信息: 给药剂量 mg/kg 动物的平均体重 g 每只动物的给药体积 μL 动物数量 只 由于实验过程有损耗,建议您多配一只动物的量 请输入您的动物体内配方组成: % DMSO + % + % Tween-80 + % Saline 如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。 方案所需 助溶剂 包括:DMSO, ,均可在 MCE 网站选购。 ,Tween 80,均可在 MCE 网站选购。 计算结果 工作液所需浓度 : mg/mL 储备液配制方法 : mg 药物溶于 μL DMSO(母液浓度为 mg/mL)。 您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。 动物实验体内工作液的配制方法 :取 μLDMSO储备液,加入 μL。 μL,混合均匀至澄清,再加 μLTween 80,混合均匀至澄清,再加 μL生理盐水。 连续给药周期超过半月以上,请谨慎选择该方案。 请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。 | ||||||||||||
纯度 & 产品资料 | 纯度: 99.85%
COA (268 KB) LCMS (273 KB) 产品使用指南 (1538 KB) | ||||||||||||
参考文献 |
|
Cell Assay [2] | GEO, HT29, SW480, and HCT116 cells are used. The effects of OSI-906 or the combination of OSI-906 and PF-4708671 on cell proliferation is determined with XTT and clonogenic assays. XTT assays are performed using the Cell Proliferation Kit II (XTT). For clonogenic assays, cells (1×103 cells/well) are seeded on a 6-well plate and subsequently treated with drugs (OSI-906 5 μM, PF-4708671 10 μM). After 1 week of incubation, cells are stained with 1% crystal violet, and the number of colonies is counted and recorded[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
---|---|
Animal Administration [2] | Mice[2] MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
|
-
[1]. Pearce LR, 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]. Zhang Y, et al. Inhibition of p70S6K1 Activation by Pdcd4 Overcomes the Resistance to an IGF-1R/IR Inhibitor in Colon Carcinoma Cells. Mol Cancer Ther. 2015 Mar;14(3):799-809.
PF-4708671 相关分类
- MAPK/ERK Pathway Autophagy
- Ribosomal S6 Kinase (RSK) Autophagy
完整储备液配制表
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。
可选溶剂 | 浓度 溶剂体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
---|
DMSO | 1 mM | 2.5614 mL | 12.8070 mL | 25.6141 mL | 64.0352 mL |
5 mM | 0.5123 mL | 2.5614 mL | 5.1228 mL | 12.8070 mL | |
10 mM | 0.2561 mL | 1.2807 mL | 2.5614 mL | 6.4035 mL | |
15 mM | 0.1708 mL | 0.8538 mL | 1.7076 mL | 4.2690 mL | |
20 mM | 0.1281 mL | 0.6404 mL | 1.2807 mL | 3.2018 mL | |
25 mM | 0.1025 mL | 0.5123 mL | 1.0246 mL | 2.5614 mL | |
30 mM | 0.0854 mL | 0.4269 mL | 0.8538 mL | 2.1345 mL | |
40 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6009 mL | |
50 mM | 0.0512 mL | 0.2561 mL | 0.5123 mL | 1.2807 mL | |
60 mM | 0.0427 mL | 0.2135 mL | 0.4269 mL | 1.0673 mL | |
80 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8004 mL |
Help & FAQs
-
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
PF-47086711255517-76-0PF4708671PF 4708671Ribosomal S6 Kinase (RSK)AutophagyS6KInhibitorinhibitorinhibit