PKI-179|cas:1197160-28-3|西域试剂

PKI-179,98.0%

产品编号：Bellancom-11080| CAS NO：1197160-28-3| 分子式：C₂₅H₂₈N₈O₃| 分子量：488.54

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货号	价格	库存与货期
Bellancom-11080	￥2500.00	杭州北京（现货）
Bellancom-11080	￥4000.00	杭州北京（现货）
Bellancom-11080	￥8000.00	杭州北京（现货）
Bellancom-11080	￥12800.00	杭州北京（现货）

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PKI-179

产品介绍

PKI-179 是一种有效的和具有口服活性的双重 PI3K/mTOR 抑制剂，对 PI3K-α，PI3K-β，PI3K-γ，PI3K-δ 和 mTOR 的 IC₅₀ 值分别为 8 nM，24 nM，74 nM，77 nM 和 0.42 nM。PKI-179 还表现出对 E545K 和 H1047R 的活性，IC₅₀ 值分别为 14 nM 和 11 nM。PKI-179 在体内显示出抗肿瘤活性。

生物活性

PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC₅₀s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC₅₀s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo.

体外研究

PKI-179 inhibits the cell proliferation, with IC₅₀s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively.
PKI-179 shows inhibitory activity against a panel of 361 other kinases, hERG and cytochrome P450 (CYP) isoforms at concentrations up to >30 μM, but does have activity for CYP2C8 (IC₅₀=3 μM).

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

体内研究

PKI-179 (5-50 mg/kg; p.o. once daily for 40 days) inhibits the tumor growth and is well tolerated in nude mice bearing MDA-361 human breast cancer tumors.
PKI-179 (50 mg/kg; p.o.) results in good inhibition of PI3K signaling in nude mice bearing MDA361 tumor xenografts.
PKI-179 exhibits good oral bioavailability (98% in nude mouse, 46% in rat, 38% in monkey, and 61% in dog) and a high half-life (>60 min) .

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

Animal Model:	Nude mice bearing MDA-361 human breast cancer tumors
Dosage:	5, 10, 25, 50 mg/kg
Administration:	I.p. every 3 days for 4 weeks
Result:	Exhibited pronounced tumor growth arrest when dosed above 10 mg/kg. No significant weight loss of tested animals was observed for all different dosages.

体内研究

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

Animal Model:	Nude mice bearing MDA-361 human breast cancer tumors
Dosage:	5, 10, 25, 50 mg/kg
Administration:	I.p. every 3 days for 4 weeks
Result:	Exhibited pronounced tumor growth arrest when dosed above 10 mg/kg. No significant weight loss of tested animals was observed for all different dosages.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (204.69 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0469 mL	10.2346 mL	20.4692 mL
5 mM	0.4094 mL	2.0469 mL	4.0938 mL
10 mM	0.2047 mL	1.0235 mL	2.0469 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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.12 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.12 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。