Gedatolisib

SKU: orb1306926

Description

Gedatolisib (PF-05212384) is a potent dual inhibitor of PI3Kα/γ and mTOR, with IC50 values of 0.4/5.4 nM and 1.6 nM, respectively. It is widely used in preclinical research to study oncogenic signaling and has demonstrated antitumor activity in both cellular assays and in vivo cancer models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1197160-78-3
• MW: 615.73
• Purity: 99.48%
• Formula: C₃₂H₄₁N₉O₄
• SMILES: N(C(NC1=CC=C(C(=O)N2CCC(N(C)C)CC2)C=C1)=O)C3=CC=C(C=4N=C(N=C(N4)N5CCOCC5)N6CCOCC6)C=C3
• Target: mTOR,PI3K
• Solubility: DMSO:10 mg/mL (16.24 mM)

Bioactivity

• Target IC50:
  PI3Kα (H1047R):0.6 nM|PI3Kδ:6 nM|mTOR:1.6 nM|PI3Kγ:5.4 nM|PI3Kα (E542K):0.6 nM|PI3Kβ:6 nM|PI3Kα:0.4 nM
• In Vivo:
  In both the MDA-361 and PC3-MM2 cell lines, PKI-587 exhibits inhibitory effects on tumor cell growth, with IC50 values of 4 and 13.1 nM, respectively. Additionally, PKI-587 is effective against mutations in PI3Kα, particularly the H1047R and E545K mutations, displaying IC50 values of 0.6 nM for both.
• In Vitro:
  In a xenograft model of H1975 non-small cell lung cancer (NSCLC) with EGFR mutations (L858R, T790M), treatment with PKI-587 at a dose of 25 mg/kg for seven days resulted in a 90% survival rate in the experimental group. PKI-587 administration (25 mg/kg, intravenously) in nude mice showed a high volume of distribution (7.2 L/kg), low plasma clearance rate (7 mL/min/kg), and an extended half-life (14.4 hours). In the MDA-361 xenograft tumor model, PKI-587 demonstrated significant antitumor activity, with the lowest effective dose being 3 mg/kg and the maximum tolerated dose at 30 mg/kg.
• Cell Research:
  Cells are plated in 96-well culture plates at about 3000 cells per well. One day following plating, PKI-587 is added to cells. Three days after PKI-587 treatment, viable cell densities are determined by measuring metabolic conversion (by viable cells) of the dye MTS, a previously established cell proliferation assay. For each assay, MTS and PMS stocks are freshly thawed and mixed (MTS/PMS, 20:1). The MTS/PMS mixture is then added to 96-well cell plates at 20 μL/well, and plates are incubated for 1 hour–2 hours in cell culture incubator. MTS assay results are read in a 96-well format plate reader by measuring absorbance at 490 nm. The effect of each PKI-587 treatment is calculated as a percentage of control cell growth obtained from vehicle-treated cells grown in the same culture plate.(Only for Reference)

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

mTOR, inhibit, Gedatolisib, Inhibitor, Mammalian target of Rapamycin, PF 05212384, PF05212384, PF-05212384, PKI 587, PKI587, PKI-587, PI3Kγ, PI3K, PI3Kα, Phosphoinositide 3-kinase

Compound Identifiers

PubChem CID

44516953