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PI-103 Hydrochloride

Catalog No. T6143L CAS 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].

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PI-103 Hydrochloride, CAS 371935-79-4

Pack Size	Availability	Price/USD	Quantity
2 mg	5 days	$ 34.00
1 mL * 10 mM (in DMSO)	5 days	$ 58.00

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Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PI-103 Hydrochloride 371935-79-4 PI103 Hydrochloride PI 103 Hydrochloride inhibitor inhibit

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