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PI-103 Hydrochloride is a potent dual inhibitor of PI3K and mTOR, demonstrating inhibitory IC50 values of 8 nM for p110α, 88 nM for p110β, 48 nM for p110δ, 150 nM for p110γ, 20 nM for mTORC1, and 83 nM for mTORC2, respectively. Additionally, it inhibits DNA-PK with an IC50 of 2 nM and induces autophagy [1] [2] [3] [4].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $34 | 5 days | |
1 mL x 10 mM (in DMSO) | $58 | 5 days |
Description | PI-103 Hydrochloride is a potent dual inhibitor of PI3K and mTOR, demonstrating inhibitory IC50 values of 8 nM for p110α, 88 nM for p110β, 48 nM for p110δ, 150 nM for p110γ, 20 nM for mTORC1, and 83 nM for mTORC2, respectively. Additionally, it inhibits DNA-PK with an IC50 of 2 nM and induces autophagy [1] [2] [3] [4]. |
In vitro | PI-103 is demonstrated to possess antiproliferative effects across various human cancer cell lines, acting essentially as a cytostatic agent by inducing cell cycle arrest in the G1 phase [1]. Additionally, it significantly inhibits leukemic proliferation, reduces the clonogenic potential of leukemic progenitors, and triggers mitochondrial apoptosis, particularly targeting the leukemic stem cell compartment [2]. It effectively targets both rapamycin-sensitive (mTORC1, IC 50=20 nM) and rapamycin-insensitive (mTORC2, IC 50=83 nM) complexes of the mTOR protein kinase, showcasing its potent inhibitory action [4]. |
In vivo | PI-103 demonstrates therapeutic efficacy against various human tumor xenografts, displaying notable inhibition of angiogenesis, invasion, metastasis, along with direct antiproliferative effects [1]. Furthermore, it induces immunosuppression which facilitates in vivo tumor growth while inhibiting apoptosis. Moreover, tumors in mice treated with PI-103 exhibit elevated levels of cyclin D1 and an increased number of proliferating cells [3]. |
Molecular Weight | 384.82 |
Formula | C19H17ClN4O3 |
Cas No. | 371935-79-4 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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