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M2698 {[allProObj[0].p_purity_real_show]}

货号:A711494 同义名: MSC2363318A

M2698是一种口服可用的丝氨酸/苏氨酸蛋白激酶(如 p70S6K 和 Akt)抑制剂,具有潜在的抗肿瘤活性。

M2698 化学结构 CAS号:1379545-95-5
M2698 化学结构
CAS号:1379545-95-5
M2698 3D分子结构
CAS号:1379545-95-5
M2698 化学结构 CAS号:1379545-95-5
M2698 3D分子结构 CAS号:1379545-95-5
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M2698 纯度/质量文件 产品仅供科研

货号:A711494 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Akt Akt1 Akt2 Akt3 其他靶点 纯度
Honokiol MEK 98%
PF-04691502 ++++

P-Akt (S473), IC50: 3.8 nM

P-Akt (T308), IC50: 7.5 nM

98+%
PHT-427 +

Akt, Ki: 2.7 μM

99%+
Deguelin PI3K 99%+
TIC10 isomer ERK 98+%
Perifosine +

Akt, IC50: 4.7 μM

98%
Miltefosine PKC,PI3K 98%
Triciribine +

Akt, IC50: 130 nM

99%+
Uprosertib +

Akt1, IC50: 180 nM

+

Akt2, IC50: 328 nM

++

Akt3, IC50: 38 nM

99%+
Afuresertib ++++

Akt1, Ki: 0.08 nM

++++

Akt2, Ki: 2 nM

++++

Akt3, Ki: 2.6 nM

99%+
Miransertib ++++

Akt1, IC50: 5 nM

++++

Akt2, IC50: 4.5 nM

++

Akt3, IC50: 16 nM

98+%
GSK-690693 ++++

Akt1, IC50: 2 nM

+++

Akt2, IC50: 13 nM

+++

Akt3, IC50: 9 nM

99%+
AT7867 ++

Akt1, IC50: 32 nM

++

Akt2, IC50: 17 nM

++

Akt3, IC50: 47 nM

PKA 99%+
AKT inhibitor VIII ++

Akt1, IC50: 58 nM

+

Akt2, IC50: 210 nM

+

Akt3, IC50: 2119 nM

97%
MK-2206 2HCl +++

Akt1, IC50: 8 nM

+++

Akt2, IC50: 12 nM

+

Akt3, IC50: 65 nM

99%+
Ipatasertib ++++

Akt1, IC50: 5 nM

++

Akt2, IC50: 18 nM

+++

Akt3, IC50: 8 nM

99%+
AT13148 ++

Akt1, IC50: 38 nM

+

Akt2, IC50: 402 nM

++

Akt3, IC50: 50 nM

PKA 95%
Capivasertib ++++

Akt1, IC50: 3 nM

+++

Akt2, IC50: 8 nM

+++

Akt3, IC50: 8 nM

99%+
A-674563 HCl +++

Akt1, Ki: 11 nM

PKA 99%
CCT128930 +++

Akt2, IC50: 6 nM

PKA 95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

M2698 生物活性

描述 M2698, an oral, ATP-competitive inhibitor, selectively targets p70S6K and Akt with IC50s of 1 nM for both p70S6K and Akt1/3. It is capable of crossing the blood-brain barrier and exhibits anti-cancer properties. At concentrations ranging from 0.3 nM to 50 M over 72 hours, M2698 dose-dependently curbs the proliferation of breast tumor cell lines, with IC50s between 0.02-8.5 µM. Additionally, at 0.3 and 1 µM for 24 hours, it inhibits p70S6K activity, triggers feedback phosphorylation on Akt, and reduces Akt activity in these cell lines. M2698 indirectly inhibits pGSK3β (IC50=17 nM) and pS6 (IC50=15 nM)[1].

M2698 动物研究

Animal study When administered orally at doses of 10-30 mg/kg/day for 28 days, M2698 achieves dose-dependent tumor growth inhibition and causes tumor regression at the maximum dose of 30 mg/kg. When administered at 20 mg/kg/day orally for 4 days, M2698 exhibits a tumor to plasma exposure ratio of 12:1 over a 24-hour period and results in elevated pAkt levels in tumor tissues. The average total concentration of M2698 following a 16-hour infusion in rats is 1750 ng/g in the brain and 175 ng/mL in plasma. Furthermore, M2698, given orally in doses of 1, 5, 10, or 20 mg/kg/day for 7 days, proportionally inhibits the phosphorylation of S6 over time, whether after a single dose or continuous daily treatments over the course of 7 days[1].

M2698 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.

M2698 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.11mL

2.22mL

1.11mL

22.23mL

4.45mL

2.22mL

M2698 技术信息

CAS号1379545-95-5
分子式C21H19ClF3N5O
分子量 449.86
SMILES Code O=C(C1=CC=CC2=C(N[C@@H](C3=CC=C(Cl)C(C(F)(F)F)=C3)CN4CCC4)N=CN=C12)N
MDL No. MFCD31744446
别名 MSC2363318A
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

DMSO: 120 mg/mL(266.75 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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案一
方案二
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