ALM301|cas:1313439-71-2|西域试剂

ALM301,99.33%

产品编号：Bellancom-151504| CAS NO：1313439-71-2| 分子式：C₂₅H₂₅N₃O₃| 分子量：415.48

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货号	价格	库存与货期
Bellancom-151504	￥4200.00	杭州北京（现货）
Bellancom-151504	￥6800.00	杭州北京（现货）
Bellancom-151504	￥13500.00	杭州北京（现货）

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ALM301

产品介绍

ALM301 是一种具有口服活性的高特异性 AKT 抑制剂，对 AKT1、AKT2 和 AKT3 的 IC₅₀ 分别 0.13 μM、0.09 μM 和 2.75 μM。ALM301 抑制 AKT 磷酸化，能在体外其调节下游信号。ALM301可抑制癌细胞增殖和肿瘤生长。

生物活性

ALM301 is an orally active highly specific AKT inhibitor with IC₅₀ values of 0.13 µM, 0.09 µM and 2.75 µM for AKT1, AKT2 and AKT3, respectively. ALM301 inhibits AKT phosphorylation and modulates downstream signalling in vitro. ALM301 can inhibit cancer cell proliferation and tumor growth.

体外研究

ALM301 (0.001-10 µM; 72 h) inhibits the proliferation of cancer cells, and PI3KCA-mutant MCF-7 cells is the most sensitive; increases sub-G0 population in a dose-dependent manner.
ALM301 (1 µM; 1 h) inhibits AKT phosphorylation in MCF-7 and sustains up to 48 h, with an EC₅₀ value of 0.47 µM.

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

Cell Proliferation Assay

Cell Line:	MCF-7, T47D, NCI-H460, HCT116 and other cancer cells
Concentration:	0.001-10 µM
Incubation Time:	72 h
Result:	Inhibited the proliferation of cancer cells, and PI3KCA-mutant MCF-7 cells was the most sensitive with an IC₅₀ of 2.25 µM.

Western Blot Analysis

Cell Line:	MCF-7
Concentration:	0.001-10 µM
Incubation Time:	1, 4, 24 and 48 h
Result:	Inhibited pAKT and pGSK3β at various concentrations and timepoints up to 48 h.

体内研究
(In Vivo)

ALM301 (10, 30 and 100 mg/kg; p.o.; single dosage) inhibits pAKT^S473 in tumors and suppresses tumor growth.
ALM301 (3 or 10 mg/kg; p.o.; q.d. for 49 days) shows better tumor inhibition ability when combined with Tamoxifen (HY-13757A).

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

Animal Model:	BALB/c mice (bearing A549 xenografts)
Dosage:	10, 30 and 100 mg/kg
Administration:	p.o.; single dosage
Result:	Increased total plasma concentrations dose-dependently that resulted in almost total abrogation of measurable pAKT^S473 in tumors at all timepoints over 24 h. Exhibited the tumour growth inhibition (TGI) of 23, 31 and 41% at 10, 30 and 100 mg/kg, respectively.

Animal Model:	BALB/c mice (bearing PIK3CA-mutant MCF-7 xenografts)
Dosage:	3 or 10 mg/kg
Administration:	p.o.; q.d. for 49 days
Result:	Showed significant tumour regressions of 57% and 50% at 3 and 10 mg/kg, respectively, when combined with Tamoxifen (HY-13757A) (5 mg/kg; q.d.).

体内研究

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

Animal Model:	BALB/c mice (bearing A549 xenografts)
Dosage:	10, 30 and 100 mg/kg
Administration:	p.o.; single dosage
Result:	Increased total plasma concentrations dose-dependently that resulted in almost total abrogation of measurable pAKT^S473 in tumors at all timepoints over 24 h. Exhibited the tumour growth inhibition (TGI) of 23, 31 and 41% at 10, 30 and 100 mg/kg, respectively.

Animal Model:	BALB/c mice (bearing PIK3CA-mutant MCF-7 xenografts)
Dosage:	3 or 10 mg/kg
Administration:	p.o.; q.d. for 49 days
Result:	Showed significant tumour regressions of 57% and 50% at 3 and 10 mg/kg, respectively, when combined with Tamoxifen (HY-13757A) (5 mg/kg; q.d.).

体内研究

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

Animal Model:	BALB/c mice (bearing A549 xenografts)
Dosage:	10, 30 and 100 mg/kg
Administration:	p.o.; single dosage
Result:	Increased total plasma concentrations dose-dependently that resulted in almost total abrogation of measurable pAKT^S473 in tumors at all timepoints over 24 h. Exhibited the tumour growth inhibition (TGI) of 23, 31 and 41% at 10, 30 and 100 mg/kg, respectively.

Animal Model:	BALB/c mice (bearing PIK3CA-mutant MCF-7 xenografts)
Dosage:	3 or 10 mg/kg
Administration:	p.o.; q.d. for 49 days
Result:	Showed significant tumour regressions of 57% and 50% at 3 and 10 mg/kg, respectively, when combined with Tamoxifen (HY-13757A) (5 mg/kg; q.d.).

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (120.34 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4069 mL	12.0343 mL	24.0685 mL
5 mM	0.4814 mL	2.4069 mL	4.8137 mL
10 mM	0.2407 mL	1.2034 mL	2.4069 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。-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: ≥ 2.5 mg/mL (6.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.02 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.02 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。