PI-103

SKU: orb1225172

Description

A potent, dual class I PI3K/mTOR inhibitor with IC50 of 2/3/3/15/ for p110α/β/δ/γ, respectively; also inhibits TORC1 (>80% inhibition at 0.5 uM) and DNA-PK (IC50=14 nM), 15- to 20-fold less activity against class II PI3K C2β (IC50=43 nM), >1,300-fold selectivity over the class III PI3K Vsp34; potently inhibits proliferation and invasion of a wide variety of human cancer cells in vitro; shows activity in cancer xenograft models.

Key Properties

• CAS Number: 371935-74-9
• MW: 348.3553
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₆N₄O₃
• SMILES: OC1=CC(=CC=C1)C1=NC2=C(OC3=C2C=CC=N3)C(=N1)N1CCOCC1 |c:3,5,13,16,18,21,t:1,8,10|
• Target: PI3K
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  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. PI-103 induces immunosuppression promoting In vivo tumor growth and inhibiting apoptosis. Tumors from PI-103-treated mice shows higher levels of cyclin D1 and more proliferating cells.
• In Vitro:
  PI-103 exhibits antiproliferative properties in a panel of human cancer cell lines. 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PI 103 | PI103

Quick Database Links

Gene Symbol

PI3K