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PI-103 Hydrochloride

CAS No. : 371935-79-4

MCE 国际站：PI-103 Hydrochloride

产品活性：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)。

研究领域：PI3K/Akt/mTOR  |  Cell Cycle/DNA Damage  |  Autophagy  |  Apoptosis

作用靶点：PI3K  |  mTOR  |  DNA-PK  |  Autophagy  |  Apoptosis

In Vitro: 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.

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. 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.

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