PI3K/mTOR Inhibitor-11|cas:2845104-25-6|西域试剂

PI3K/mTOR Inhibitor-11,98.74%

产品编号：Bellancom-151622| CAS NO：2845104-25-6| 分子式：C₂₇H₂₁N₇| 分子量：443.50

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-151622		￥5400.00	杭州北京（现货）
Bellancom-151622		￥8500.00	杭州北京（现货）

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PI3K/mTOR Inhibitor-11

产品介绍

PI3K/mTOR Inhibitor-11 是一种具有口服活性的 PI3K/mTOR 抑制剂 (对 PI3Kα、PI3Kδ 和 mTOR 的 IC₅₀ 分别为 3.5、4.6 和 21.3 nM)。PI3K/mTOR Inhibitor-11 通过抑制 AKT 和 S6 蛋白的磷酸化来调节 PI3K/AKT/mTOR 信号通路。PI3K/mTOR Inhibitor-11 可用于癌症研究。

生物活性

PI3K/mTOR Inhibitor-11 is an orally active PI3K/mTOR inhibitor (IC₅₀: 3.5, 4.6, and 21.3 nM for PI3Kα, PI3Kδ, and mTOR). PI3K/mTOR Inhibitor-11 regulates the PI3K/AKT/mTOR signaling pathway by inhibiting the phosphorylation of AKT and S6 proteins. PI3K/mTOR Inhibitor-11 can be used in the research of cancers.

体外研究

PI3K/mTOR Inhibitor-11 (compound 8o) inhibits various human cancer cell lines HT29, HCT15, H3122, HeLa, SW620, and H446 viability with IC₅₀ values of 0.25, 0.17, 0.29, 0.09, 0.16, and 0.97 μM, respectively.
PI3K/mTOR Inhibitor-11 (0-1.25 μM, 15 days) decreases the colony formation rates of HeLa and SW620 cells.
PI3K/mTOR Inhibitor-11 (0-2.5 μM, 24 h) arrests HeLa and SW620 cells at the G0/G1 phases.
PI3K/mTOR Inhibitor-11 (0-2.5 μM, 24 h) suppressees the phosphorylated AKT and S6 proteins in HeLa cells.

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

Apoptosis Analysis

Cell Line:	HeLa and SW620 cells
Concentration:	0, 0.15625, 0.625, 1.25 μM
Incubation Time:	24 h
Result:	Affected HeLa cells’ apoptosis rate from 6.10 to 66.04% in a dose-dependent manner.

Western Blot Analysis

Cell Line:	HeLa
Concentration:	0, 0.15625, 0.625, 1.25, 2.5 μM
Incubation Time:	24 h
Result:	Suppressed the phosphorylated AKT (Ser473 and Thr308) and S6 proteins.

体内研究
(In Vivo)

PI3K/mTOR Inhibitor-11 (compound 8o, 15-60 mg/kg, intragastric administration) suppresses the growth of HeLa and SW620 xenograft tumors.
PI3K/mTOR Inhibitor-11 (1 mg/kg for i.v., 10 mg/kg for p.o., rats) shows oral bioavailability (76.81%).

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

Animal Model:	HeLa and SW620 xenograft models of female BALB/c nude mice.
Dosage:	15, 30, and 60 mg/kg
Administration:	Intragastric administration, daily for 30 days.
Result:	The TGIs (tumor growth inhibitions): 80.22, 73.50, and 60.79% in the HeLa xenograft model at doses of 60, 30, and 15 mg/kg, respectively. TGIs: 81.03, 70.81, and 60.58% in the SW620 xenograft model at doses of 60, 30, and 15 mg/kg, respectively.

Animal Model:

Rats.

Dosage:

1 mg/kg for i.v., 10 mg/kg for p.o.

Administration:

i.v., p.o.

Result:

Pharmacokinetic parameters of PI3K/mTOR Inhibitor-11 (compound 8o)

dose (mg/kg)	T_1/2 (h)	C_max (ng/mL)	CL (mL/min/kg)	F (%)
1 (i.v.)			17.2
10 (p.o.)	2.6	2995		76.81%

体内研究

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

Animal Model:	HeLa and SW620 xenograft models of female BALB/c nude mice.
Dosage:	15, 30, and 60 mg/kg
Administration:	Intragastric administration, daily for 30 days.
Result:	The TGIs (tumor growth inhibitions): 80.22, 73.50, and 60.79% in the HeLa xenograft model at doses of 60, 30, and 15 mg/kg, respectively. TGIs: 81.03, 70.81, and 60.58% in the SW620 xenograft model at doses of 60, 30, and 15 mg/kg, respectively.

Animal Model:

Rats.

Dosage:

1 mg/kg for i.v., 10 mg/kg for p.o.

Administration:

i.v., p.o.

Result:

Pharmacokinetic parameters of PI3K/mTOR Inhibitor-11 (compound 8o)

dose (mg/kg)	T_1/2 (h)	C_max (ng/mL)	CL (mL/min/kg)	F (%)
1 (i.v.)			17.2
10 (p.o.)	2.6	2995		76.81%

体内研究

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

Animal Model:	HeLa and SW620 xenograft models of female BALB/c nude mice.
Dosage:	15, 30, and 60 mg/kg
Administration:	Intragastric administration, daily for 30 days.
Result:	The TGIs (tumor growth inhibitions): 80.22, 73.50, and 60.79% in the HeLa xenograft model at doses of 60, 30, and 15 mg/kg, respectively. TGIs: 81.03, 70.81, and 60.58% in the SW620 xenograft model at doses of 60, 30, and 15 mg/kg, respectively.

Animal Model:

Rats.

Dosage:

1 mg/kg for i.v., 10 mg/kg for p.o.

Administration:

i.v., p.o.

Result:

Pharmacokinetic parameters of PI3K/mTOR Inhibitor-11 (compound 8o)

dose (mg/kg)	T_1/2 (h)	C_max (ng/mL)	CL (mL/min/kg)	F (%)
1 (i.v.)			17.2
10 (p.o.)	2.6	2995		76.81%

性状

Solid

溶解性数据

In Vitro:

DMSO : 40 mg/mL (90.19 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2548 mL	11.2740 mL	22.5479 mL
5 mM	0.4510 mL	2.2548 mL	4.5096 mL
10 mM	0.2255 mL	1.1274 mL	2.2548 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)。-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 90% corn oil
Solubility: ≥ 4 mg/mL (9.02 mM); Clear solution

此方案可获得 ≥ 4 mg/mL (9.02 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 40.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。