M2698 MSC2363318A|cas:1379545-95-5|西域试剂

M2698 MSC2363318A,99.81%

产品编号：Bellancom-100501| CAS NO：1379545-95-5| 分子式：C₂₁H₁₉ClF₃N₅O| 分子量：449.86

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货号	价格	库存与货期
Bellancom-100501	￥2200.00	杭州北京（现货）
Bellancom-100501	￥3500.00	杭州北京（现货）
Bellancom-100501	￥7000.00	杭州北京（现货）
Bellancom-100501	￥11500.00	杭州北京（现货）

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M2698 MSC2363318A

产品介绍

M2698 (MSC2363318A) 是一种具有口服活性，ATP 竞争的，选择性的 p70S6K 和 Akt 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。

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.

体外研究

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.
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.
M2698 inhibits indirectly pGSK3β (IC₅₀=17 nM) and pS6 (IC₅₀=15 nM).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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

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.
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.
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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female nude mice bearing MDA-MB-468 tumors
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
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	Daily; for 4 days
Result:	Had a tumor:plasma exposure ratio of 12:1 over 24 hours.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female nude mice bearing MDA-MB-468 tumors
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
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	Daily; for 4 days
Result:	Had a tumor:plasma exposure ratio of 12:1 over 24 hours.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female nude mice bearing MDA-MB-468 tumors
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
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	Daily; for 4 days
Result:	Had a tumor:plasma exposure ratio of 12:1 over 24 hours.

性状

Solid

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。