M2698(Synonyms: MSC2363318A)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

M2698 (Synonyms: MSC2363318A) 纯度: 99.74%

M2698 (MSC2363318A) 是一种具有口服活性,ATP 竞争的,选择性的 p70S6KAkt 双重抑制剂,对于 p70S6K,Akt1 和 Akt3 的 IC50 均为 1 nM。M2698 可以透过血脑屏障,具有抗癌活性。

M2698(Synonyms: MSC2363318A)

M2698 Chemical Structure

CAS No. : 1379545-95-5

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M2698 相关产品

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生物活性

M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity[1].

IC50 & Target[1]

p70S6K

1 nM (IC50)

Akt1

1 nM (IC50)

Akt3

1 nM (IC50)

体外研究
(In Vitro)

M2698 (0.3 nM to 50 M; 72 hours) inhibits proliferation in a dose-dependent manner in breast tumors cell lines with IC50s of 0.02-8.5 µM[1].
M2698 (0.3, 1 µM; 24 hours) inhibits p70S6K activity and induces feedback loop phosphorylation on Akt and suppresses Akt activity in breast cancer cell lines[1].
M2698 inhibits indirectly pGSK3β (IC50=17 nM) and pS6 (IC50=15 nM)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Breast tumors cell lines
Concentration: 0.3 nM to 50 M
Incubation Time: 72 hours
Result: Inhibited proliferation in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: HCC1419 and MDA-MB-453 cells
Concentration: 0.3, 1 µM
Incubation Time: 24 hours
Result: Inhibited p70S6K activity and induced feedback loop phosphorylation on Akt and suppressed Akt activity in breast cancer cell lines.

体内研究
(In Vivo)

M2698 (10-30 mg/kg/day; PO; 28 days) results in dose-dependent inhibition of tumor growth and results in tumor regression with the highest dose of 30 mg/kg[1].
M2698 (20 mg/kg/day; PO; 4 days) has a tumor:plasma exposure ratio of 12:1 over 24 hours and leads to increased levels of pAkt in tumor tissue[1].
The mean total concentration of M2698 after 16-hour infusion in rats is 1750 ng/g and 175 ng/mL in brain and plasma, respectively[1].
M2698 (po; 1, 5, 10, or 20 mg/kg/day; for 7 days) inhibits the phosphorylation of S6 in a dose-proportional manner over time after a single administration or daily treatments over 7 days[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice bearing MDA-MB-468 tumors[1]
Dosage: 10, 20 and 30 mg/kg
Administration: PO; daily; for 28 days
Result: Resulted in dose-dependent inhibition of tumor growth and resulted in tumor regression with the highest dose of 30 mg/kg.
Animal Model: Female SCID Beige mice with MDA-MB-453 xenografted[1]
Dosage: 20 mg/kg (Pharmacokinetic Analysis)
Administration: Daily; for 4 days
Result: Had a tumor:plasma exposure ratio of 12:1 over 24 hours.

Clinical Trial

分子量

449.86

Formula

C21H19ClF3N5O

CAS 号

1379545-95-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : 125 mg/mL (277.86 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2229 mL 11.1146 mL 22.2291 mL
5 mM 0.4446 mL 2.2229 mL 4.4458 mL
10 mM 0.2223 mL 1.1115 mL 2.2229 mL

*

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 (protect from light, stored under nitrogen)。-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。

In Vivo:

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:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.62 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.62 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.62 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.62 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Machl A, et al. M2698 is a potent dual-inhibitor of p70S6K and Akt that affects tumor growth in mouse models of cancer and crosses the blood-brain barrier. Am J Cancer Res. 2016 Mar 15;6(4):806-18.

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