ETP-46464

SKU: orb1306518

Description

ETP-46464

Research Area

Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 1345675-02-6
• MW: 470.52
• Purity: 99.56%
• Formula: C₃₀H₂₂N₄O₂
• SMILES: CC(C)(C#N)c1ccc(cc1)N1C(=O)OCc2cnc3ccc(cc3c12)-c1cnc2ccccc2c1
• Target: PI3K,ATM/ATR,mTOR,DNA-PK
• Solubility: DMSO:6 mg/mL (12.75 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  ATM:545 nM|ATR:25nM|mTOR:0.6 nM|PI3Kα:170 nM|DNA-PK:36 nM
• In Vivo:
  ETP-46464 (1 μM) exhibits inhibitory effects on the G2/M phase checkpoint induced by ionizing radiation, resulting in cells with micronuclei or completely fragmented nuclei. It significantly enhances the toxicity in p53-deficient cells, particularly under replicative stress conditions like cyclin E overexpression, intensifying the toxicity. At a concentration of 100 nM, ETP-46464 can fully inhibit ATR activity. Furthermore, ETP-46464 inhibits the activity of PI3Kα (IC50: 170 nM), mTOR (IC50: 0.6 nM), and DNA-PKcsmTOR (IC50: 36 nM) proteins. It promotes damage due to replication fork stalling and induces extensive DNA damage in replicating cells.

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

Inhibitor, inhibit, mTOR, ETP-46464, ETP 46464, ETP46464, Mammalian target of Rapamycin, ATM, ATM/ATR, ATM and RAD3 related, Ataxia telangiectasia mutated, ATR, DNA-PK, DNAPK, PI3Kα

Compound Identifiers

PubChem CID

72199292