PI-103 Hydrochloride|cas:371935-79-4|西域试剂

PI-103 Hydrochloride,98.00%

产品编号：Bellancom-10115A| CAS NO：371935-79-4| 分子式：C₁₉H₁₇ClN₄O₃| 分子量：384.82

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货号	价格	库存与货期
Bellancom-10115A	￥990.00	杭州北京（现货）
Bellancom-10115A	￥1550.00	杭州北京（现货）
Bellancom-10115A	￥3464.00	杭州北京（现货）
Bellancom-10115A	￥4201.00	杭州北京（现货）

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PI-103 Hydrochloride

产品介绍

PI-103 Hydrochloride 是一种有效的 PI3K 和 mTOR 抑制剂，抑制 p110α，p110β，p110δ，p110γ，mTORC1 和 mTORC2，IC₅₀ 分别为 8 nM，88 nM，48 nM，150 nM，20 nM 和 83 nM。PI-103 Hydrochloride 也可抑制DNA-PK，IC₅₀ 为 2 nM。PI-103 Hydrochloride 诱导自噬 (autophagy)。

生物活性

PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC₅₀s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy^[4].

体外研究

PI-103 exhibits antiproliferative properties in a panel of human cancer cell lines. PI-103 is essentially cytostatic for cell lines and induced cell cycle arrest in the G1 phase. In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis, especially in the compartment containing leukemic stem cells . PI-103 potently inhibits both the rapamycin-sensitive (mTORC1, IC₅₀=20 nM) and rapamycin-insensitive (mTORC2, IC₅₀=83 nM) complexes of the protein kinase mTOR^[4].

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

体内研究

PI-103 shows therapeutic activity against a range of human tumor xenografts, exhibiting inhibition of angiogenesis, invasion, and metastasis, as well as direct antiproliferative effects. PI-103 induces immunosuppression promoting in vivo tumor growth and inhibiting apoptosis. Tumors from PI-103-treated mice shows higher levels of cyclin D1 and more proliferating cells.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 4.1 mg/mL (10.65 mM; Need ultrasonic and warming)

H₂O : 1 mg/mL (2.60 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	2.5986 mL	12.9931 mL	25.9862 mL
5 mM	0.5197 mL	2.5986 mL	5.1972 mL
10 mM	0.2599 mL	1.2993 mL	2.5986 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 (sealed storage, away from moisture)。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献