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Apitolisib

Catalog No. T1916   CAS 1032754-93-0
Synonyms: RG 7422, GNE 390, GDC-0980

Apitolisib (RG 7422), an effective, class I PI3K inhibitor for PI3Kα(IC50=5 nM), PI3Kβ(IC50=27 nM), PI3Kδ(IC50=7 nM), PI3Kγ (IC50=14 nM), is used in trials study of solid cancers, breast cancer, prostate cancer, renal cell carcinoma, and endometrial carcinoma, among others.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Apitolisib Chemical Structure
Apitolisib, CAS 1032754-93-0
Pack Size Availability Price/USD Quantity
2 mg In stock $ 38.00
5 mg In stock $ 58.00
10 mg In stock $ 88.00
25 mg In stock $ 159.00
50 mg In stock $ 258.00
100 mg In stock $ 423.00
1 mL * 10 mM (in DMSO) In stock $ 63.00
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Purity: 99.52%
Purity: 98.28%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Apitolisib (RG 7422), an effective, class I PI3K inhibitor for PI3Kα(IC50=5 nM), PI3Kβ(IC50=27 nM), PI3Kδ(IC50=7 nM), PI3Kγ (IC50=14 nM), is used in trials study of solid cancers, breast cancer, prostate cancer, renal cell carcinoma, and endometrial carcinoma, among others.
Targets&IC50 p110α:5 nM, p110γ:14 nM, p110δ:7 nM
Kinase Assay Enzymatic activity: Enzymatic activity of the Class I PI3K isoforms is measured using a fluorescence polarization assay that monitors formation of the product 3,4,5-inositoltriphosphate molecule as it competes with fluorescently labeled PIP3 for binding to the GRP-1 pleckstrin homology domain protein. An increase in phosphatidyl inositide-3-phosphate product results in a decrease in fluorescence polarization signal as the labeled fluorophore is displaced from the GRP-1 protein binding site. Class I PI3K isoforms are expressed and purified as heterodimeric recombinant proteins. PI3K isoforms are assayed under initial rate conditions in the presence of 10 mM Tris (pH 7.5), 25 μM ATP, 9.75 μM PIP2, 5% glycerol, 4 mM MgCl2, 50 mM NaCl, 0.05% (v/v) Chaps, 1 mM dithiothreitol, 2% (v/v) DMSO at the following concentrations for each isoform: PI3Kα,β at 60 ng/mL; PI3Kγ at 8 ng/mL; PI3Kδ at 45 ng/mL. After assay for 30 minutes at 25°C, reactions are terminated with a final concentration of 9 mM EDTA, 4.5 nM TAMRA-PIP3, and 4.2 μg/mL GRP-1 detector protein before reading fluorescence polarization on an Envision plate reader. IC50s are calculated from the fit of the dose?response curves to a 4-parameter equation.Human recombinant mTOR(1360?2549) is expressed and purified from insect cells and assayed using a Lanthascreen fluorescence resonance energy transfer format in which phosphorylation of recombinant green fluorescent protein (GFP)-4-EBP1 is detected using a terbium-labeled antibody to phospho-threonine 37/46 of 4-EBP1. Reactions are initiated with ATP and conducted in the presence of 50 mM Hepes (pH 7.5), 0.25 nM mTOR, 400 nM GFP-4E-BP1, 8 μM ATP, 0.01% (v/v) Tween 20, 10 mM MnCl2, 1 mM EGTA, 1 mM dithiothreitol, and 1% (v/v) DMSO. Assays are conducted under initial rate conditions at room temperature for 30 minutes before terminating the reaction and detecting product in the presence of 2 nM Tb-anti-p4E-BP1 antibody and 10 mM EDTA.Dose?response curves are fit to an equation for competitive tight-binding inhibition and apparent Ki' s are calculated using the determined Km for ATP of 6.1 μM.
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)
Synonyms RG 7422, GNE 390, GDC-0980
Molecular Weight 498.6
Formula C23H30N8O3S
CAS No. 1032754-93-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 16 mg/mL (32.1 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Sutherlin DP, et al. J Med Chem, 2011, 54(21), 7579-7587. 2. Wallin JJ, et al. Mol Cancer Ther, 2011, 10(12), 2426-2436. 3. Makhov PB, et al. 2012. doi: 10.1158/1535-7163. MCT-11-0907.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Metabolism Compound Library Anti-Lung Cancer Compound Library Anti-Aging Compound Library Neural Regeneration Compound Library Glycolysis Compound Library Anti-Cancer Compound Library Anti-Metabolism Disease Compound Library

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Keywords

Apitolisib 1032754-93-0 Apoptosis PI3K/Akt/mTOR signaling PI3K mTOR GNE-390 RG 7422 inhibit GNE 390 GDC-0980 Inhibitor RG-7422 GDC0980 Phosphoinositide 3-kinase GNE390 GDC 0980 Mammalian target of Rapamycin RG7422 inhibitor

 

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