PI-103 Hydrochloride 是一种有效的PI3K和mTOR双重抑制剂，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 诱导细胞自噬 (Autophagy)。

PI-103 Hydrochloride is a potent and dual inhibitor of PI3K and mTOR with IC 50 s 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 [1] [2] [3] [4].

PI-103 shows 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, IC 50 =20 nM) and rapamycin-insensitive (mTORC2, IC 50 =83 nM) complexes of the protein kinase mTOR [4].

PI-103 shows therapeutic activity against a range of human tumor xenografts, exhibiting inhibition of angiogenesis, invasion, metastasis, and direct antiproliferative effects [1]. 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 [3].

371935-79-4

C19H17ClN4O3

384.82

PI-103 Hydrochloride

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years