GNE-477

SKU: orb1227107

Description

A potent, dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Ki of 21 nM for mTOR; inhibits MCF7.1 cell proliferation with EC50 of 143 nM; displays desirable pharmacokinetic properties, exhibits stasis in a PC3 tumor growth inhibition study.

Key Properties

• CAS Number: 1032754-81-6
• MW: 504.6288
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₈N₈O₃S₂
• SMILES: NC1=NC=C(C2=NC(N3CCOCC3)=C4C(C(C)=C(CN5CCN(S(=O)(C)=O)CC5)S4)=N2)C=N1
• Target: PI3K
• Solubility: DMSO: < 9.2 mg/mL

Bioactivity

• In Vivo:
  GNE-477 also exhibits stasis in a PC3 tumor growth inhibition study. In an experiment evaluating the tumor growth inhibition of a PC3 tumor xenograft over 14 days, stasis is achieved at a 20 mg/kg QD dose and significant inhibition is observed with doses as low as 1 mg/kg QD. GNE-477 is generally well tolerated during this study as demonstrated by acceptable levels of weight loss comparable to that observed with the animals in the vehicle cohort.

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

GNE477 | GNE 477

Quick Database Links

Gene Symbol

PI3K