PI-103 Hydrochloride

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CAS NO:

371935-79-4

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

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 dualPI3KandmTORinhibitor withIC₅₀s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM forp110α,p110β,p110δ,p110γ,mTORC1, andmTORC2. PI-103 Hydrochloride also inhibitsDNA-PKwith anIC50of 2 nM. PI-103 Hydrochloride inducesautophagy^[1]^[2]^[3]^[4].

IC₅₀& Target

p110α

2 nM (IC₅₀)

p110β

3 nM (IC₅₀)

p110δ

3 nM (IC₅₀)

p110γ

15 nM (IC₅₀)

mTORC1

20 nM (IC₅₀)

mTORC2

83 nM (IC₅₀)

DNA-PK

23 nM (IC₅₀)

体外研究
(In Vitro)

PI-103 exhibits antiproliferative properties in a panel of human cancer cell lines^[1]. 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^[2]. 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].

体内研究
(In Vivo)

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^[1]. PI-103 induces immunosuppression promotingin vivotumor growth and inhibiting apoptosis. Tumors from PI-103-treated mice shows higher levels of cyclin D1 and more proliferating cells^[3].

分子量

384.82

性状

Solid

Formula

C₁₉H₁₇ClN₄O₃

CAS 号

371935-79-4

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)

溶解性数据

In Vitro:

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

H₂O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble)

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。