Apitolisib

SKU: orb1307117

Description

Apitolisib

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1032754-93-0
• MW: 498.6
• Purity: 99.64%
• Formula: C₂₃H₃₀N₈O₃S
• SMILES: C[C@H](O)C(=O)N1CCN(Cc2sc3c(nc(nc3c2C)-c2cnc(N)nc2)N2CCOCC2)CC1
• Target: PI3K,Apoptosis,mTOR
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:4.99 mg/mL (10.01 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.01 mM)

Bioactivity

• Target IC50:
  PI3Kβ:27 nM|p110δ:7 nM|p110γ:14 nM|p110α:5 nM|mTOR:17 nM (Ki)
• In Vivo:
  In PC3 (IC50=307 nM) and MCF7 cells (IC50=255 nM), GDC-0980 significantly inhibited cell proliferation. For class I PI3K and mTOR kinases, the selective inhibitory effect of GDC-0980 was significant for mTOR (Ki=17 nM), for PI3Kα (IC50=5 nM), β (IC50=27 nM), δ (IC50=7 nM), and γ (IC50=14 nM).
• In Vitro:
  In PC3 (IC50=307 nM) and MCF7 cells (IC50=255 nM), GDC-0980 significantly inhibited cell proliferation. For class I PI3K and mTOR kinases, the selective inhibitory effect of GDC-0980 was significant for mTOR (Ki=17 nM), for PI3Kα (IC50=5 nM), β (IC50=27 nM), δ (IC50=7 nM), and γ (IC50=14 nM).
• Cell Research:
  Antiproliferative cellular assays are conducted using PC3 and MCF7.1 human tumor cell lines. MCF7.1 is an in vivo selected line and originally derived from the parental human MCF7 breast cancer cell line. Cell lines are cultured in RPMI supplemented with 10% fetal bovine serum, 100 units/mL penicillin, and 100 μg/mL streptomycin, 10 mM HEPES, and 2 mM glutamine at 3°C under 5% CO2. MCF7.1 cells or PC3 cells are seeded in 384-well plates in media at 1000 cells/well or 3000 cells/well, respectively, and incubated overnight prior to the addition of GDC-0980 to a final DMSO concentration of 0.5% v/v. MCF7.1 cells and PC3 cells are incubated for 3 days and 4 days, respectively, prior to the addition of CellTiter-Glo reagen and reading of luminescence using an Analyst plate reader. For antiproliferative assays, a cytostatic agent such as aphidicolin and a cytotoxic agent such as staurosporine are included as controls. Dose response curves are fit to a 4-parameter equation and relative IC50s are calculated using Assay Explorer software.(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

GDC0980, GDC-0980, GDC 0980, Mammalian target of Rapamycin, GNE390, GNE-390, GNE 390, inhibit, mTOR, Inhibitor, Apoptosis, Apitolisib, RG 7422, RG7422, RG-7422, p110β, p110α, p110δ, p110γ, PI3K, Phosphoinositide 3-kinase

Compound Identifiers

PubChem CID

25254071