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].

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].

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].

384.82

Solid

C₁₉H₁₇ClN₄O₃

371935-79-4

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

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

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

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

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。