PKI-402

SKU: orb1693625

Description

PKI-402 is a highly potent dual inhibitor of PI3K and mTOR, demonstrating low nanomolar IC50 values against key isoforms including PI3Kα (2 nM) and mTOR (3 nM). It is a valuable research tool for investigating the PI3K/Akt/mTOR signaling pathway in cancer and other diseases, with utility in both in vitro and in vivo experimental models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1173204-81-3
• MW: 570.65
• Purity: 99.94%
• Formula: C₂₉H₃₄N₁₀O₃
• SMILES: CCn1nnc2c(nc(nc12)-c1ccc(NC(=O)Nc2ccc(cc2)C(=O)N2CCN(C)CC2)cc1)N1CCOCC1
• Target: PI3K,mTOR
• Solubility: DMSO:5 mg/mL (8.76 mM)

Bioactivity

• Target IC50:
  PI3Kδ:14 nM|PI3Kα (H1047R):3 nM|PI3Kγ:16 nM|mTOR:3 nM|PI3Kα:2 nM|PI3Kβ:7 nM|PI3Kα (E542K):3 nM
• In Vivo:
  PKI-402 exhibits antitumor efficacy via intravenous administration in breast [MDA-MB-361: Her2+ and PIK3CA (E545K)], glioma (U87MG and PTEN), and NSCLC (A549; K-Ras and STK11) xenograft models, with induced regression observed specifically in the MDA-MB-361 model.
• In Vitro:
  PKI-402 causes in vitro growth inhibition of human tumor cell lines derived from a diverse set of human tumor tissues, including breast, brain (glioma), pancreas, and non-small cell lung cancer (NSCLC) tissues.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PKI402, PKI-402, PKI 402

Compound Identifiers

PubChem CID

44187953