PI-103 Hydrochloride

SKU: orb1909002

Description

PI-103 Hydrochloride is a dual PI3K/Akt and mTOR inhibitor that potently targets multiple kinases including p110 isoforms, DNA-PK, and mTOR complexes at nanomolar concentrations. It induces autophagy, mitochondrial apoptosis, and cell cycle arrest, making it a valuable tool for studying leukemia mechanisms in both cellular and animal models.

Research Area

Cell Biology, Metabolism Research, Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 371935-79-4
• MW: 384.82
• Formula: C₁₉H₁₇ClN₄O₃
• SMILES: Cl.Oc1cccc(c1)-c1nc(N2CCOCC2)c2oc3ncccc3c2n1
• Target: Others
• Solubility: DMSO:3 mg/mL (7.8 mM);H2O:< 1 mg/mL (insoluble)

Bioactivity

• Target IC50:
  mTORC2:83 nM|p110β:3 nM|DNA-PK:23 nM|mTORC1:20 nM|p110δ:3 nM|p110α:2 nM|p110γ:15 nM
• In Vivo:
  An orthotopic xenograft model was established by subcutaneously injecting 37-31E-F3 melanoma cells into immunocompetent FVB/N wild-type mice. Subsequent drug administration to the mice showed the following results: PI-103 Hydrochloride (10 mg/kg) significantly promoted in vivo tumor growth, while sorafenib (50 mg/kg) inhibited tumor growth. Compared with sorafenib monotherapy, the combined treatment with the two drugs did not exhibit additional benefits in terms of tumor inhibitory effect; furthermore, the tumor volume in the combined treatment group was even slightly larger than that in the sorafenib monotherapy group .
  Read more...
• In Vitro:
  PI-103 Hydrochloride exhibits anti-proliferative properties in a panel of Homo sapiens cancer cell lines (including prostate cancer, ovarian cancer, glioblastoma, and oropharyngeal squamous cell carcinoma) as well as in Homo sapiens umbilical vein endothelial cells . PI-103 Hydrochloride demonstrates dose-dependent inhibition of proliferation in 37-31E and 37-31E-F3 cells. For 37-31E cells, proliferation growth can be inhibited by 50% when the PI-103 Hydrochloride concentration exceeds 100 nM, whereas the concentration required to achieve 50% inhibition in 37-31E-F3 cells is 40±2 nM. In the 37-31E-F3 cell line, the inhibitory effects of PI-103 Hydrochloride at concentrations of 50 nM and 100 nM are comparable to those achieved with 500 nM PI-103 Hydrochloride in the 37-31E cell line .
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PI 103 Hydrochloride, PI103 HCl, PI-103 Hydrochloride

Compound Identifiers

PubChem CID

16739368