mTOR inhibitor-3

SKU: orb1309384

Description

mTOR inhibitor-3

Research Area

Pharmacology & Drug Discovery; Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1207358-59-5
• MW: 474.56
• Purity: 98.14% (May vary between batches)
• Formula: C₂₅H₃₀N₈O₂
• SMILES: CCNC(=O)Nc1ccc(cc1)-c1nc2CN(CCc2c(n1)N1CCOC[C@@H]1C)c1ncccn1
• Target: mTOR
• Solubility: DMSO:40 mg/mL (84.29 mM)

Bioactivity

• Target IC50:
  mTOR:1.5 nM (ki)
• In Vivo:
  mTOR inhibitor-3 achieves tumor stasis at the highest 200 mg/kg/day dose examined, which appears to also be approaching the limit of tolerability for this molecule. Plasma levels of mTOR inhibitor-3 6 h following oral administration in PC3 tumor-bearing mice along with the fold decreases of phosphorylated mTORC1 and -2 substrates relative to time-matched vehicle controls.mTOR inhibitor-3 has moderate terminal elimination half-life (t1/2=1.7 h for mouse(1 mg/kg, iv)).
• In Vitro:
  mTOR inhibitor-3 is an mTOR inhibitsor(Ki of 1.5 nM), 500-fold selectivity over closely related PI3 kinases. mTOR inhibitor-3 inhibits NCI-PC3 and MCF7neo/Her2 cells proliferation with IC50s of 150 nM and 57 nM, respectively.

Storage & Handling

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

Alternative Names

Inhibitor, inhibit, mTOR inhibitor 3, mTOR inhibitor3, mTOR inhibitor-3, mTOR, Mammalian target of Rapamycin

Compound Identifiers

PubChem CID

59239114