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PI-103 Hydrochloride

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Catalog No. T6143LCas No. 371935-79-4

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].

PI-103 Hydrochloride

PI-103 Hydrochloride

😃Good
Catalog No. T6143LCas No. 371935-79-4
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 SizePriceAvailabilityQuantity
2 mg$345 days
1 mL x 10 mM (in DMSO)$585 days
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight384.82
FormulaC19H17ClN4O3
Cas No.371935-79-4
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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