Apitolisib - CAS 1032754-93-0
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Not Intended for Therapeutic Use. For research use only.
Apitolisib, also known as GDC-0980 and RG7422;  or GNE390, is a dual PI3 kinase/mTOR inhibitor,   is also an orally available agent targeting phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinase in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. PI3K/mTOR kinase inhibitor GDC-0980 inhibits both PI3K kinase and mTOR kinase, which may result in tumor cell apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated in a PI3K-independent fashion.
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GDC-0980; GDC0980; GDC 0980; RG7422; RG-7422; RG 7422; GNE 390; GNE390; GNE-390; Apitolisib
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1.Phase I Study of Apitolisib (GDC-0980), Dual Phosphatidylinositol-3-Kinase and Mammalian Target of Rapamycin Kinase Inhibitor, in Patients with Advanced Solid Tumors.
Dolly SO1, Wagner AJ2, Bendell JC3, Kindler HL4, Krug LM5, Seiwert TY4, Zauderer MG5, Lolkema MP6, Apt D7, Yeh RF7, Fredrickson JO7, Spoerke JM7, Koeppen H7, Ware JA7, Lauchle JO7, Burris HA3, de Bono JS8. Clin Cancer Res. 2016 Jan 19. [Epub ahead of print]
PURPOSE: This first-in-human phase I trial assessed the safety, tolerability, and preliminary antitumor activity of apitolisib (GDC-0980), a dual inhibitor of class I PI3K, and mTOR kinases.
2.A supported liquid extraction-LC-MS/MS method for determination of GDC-0980 (Apitolisib), a dual small-molecule inhibitor of class 1A phosphoinositide 3-kinase and mammalian target of rapamycin, in human plasma.
Ding X1, Li F2, McKnight J2, Schmidt C2, Strooisma K2, Shimizu H3, Faber K4, Ware JA4, Dean B5. J Pharm Biomed Anal. 2014 Nov;100:150-6. doi: 10.1016/j.jpba.2014.08.001. Epub 2014 Aug 10.
A liquid chromatographic-tandem mass spectrometry (LC-MS/MS) method for the determination of GDC-0980 (Apitolisib) concentrations in human plasma has been developed and validated to support clinical development. Supported liquid extraction (SLE) was used to extract plasma samples (80μL) and the resulting samples were analyzed using reverse-phase chromatography and mass spectrometry coupled with a turbo-ionspray interface. The mass analysis of GDC-0980 was performed using multiple reaction monitoring (MRM) transitions in positive ionization mode. The method was validated over the calibration curve range 0.0500-25.0ng/mL using linear regression and 1/x(2) weighting. Within-run relative standard deviation (%RSD) ranged from 0.4 to 3.9%, while the between-run %RSD varied from 1.1 to 1.5% for QCs. The accuracy ranged from 96.1% to 106.7% of nominal for within-run and 96.7-106.7% of nominal for between-run at all concentrations including the LLOQ quality control at 0.
3.Determination of GDC-0980 (apitolisib), a small molecule dual phosphatidylinositide 3-kinase/mammalian target of rapamycin inhibitor in dog plasma by LC-MS/MS to support a GLP toxicology study.
Ding X1, Salphati L1, Kim A2, Morinello E2, Wong L2, Pang J1, Percey S3, Meng M3, Reuschel S3, Dean B1. Biomed Chromatogr. 2015 Aug;29(8):1274-9. doi: 10.1002/bmc.3417. Epub 2015 Feb 10.
An LC-MS/MS method for the determination of GDC-0980 (apitolisib) concentrations in dog plasma has been developed and validated for the first time to support pre-clinical drug development. Following protein precipitation with acetonitrile, the resulting samples were analyzed using reverse-phase chromatography on a Metasil AQ column. The mass analysis was performed on a triple quadruple mass spectrometer coupled with an electrospray interface in positive ionization mode. The selected reaction monitoring transitions monitored were m/z 499.3 → 341.1 for GDC-0980 and m/z 507.3 → 341.1 for IS. The method was validated over the calibration curve range 0.250-250 ng/mL with linear regression and 1/x(2) weighting. Relative standard deviation (RSD) ranged from 0.0 to 10.9% and accuracy ranged from 93.4 to 113.6% of nominal. Stable-labeled internal standard GDC-0980-d8 was used to minimize matrix effects. This assay was used for the measurement of GDC-0980 dog plasma concentrations to determine toxicokinetic parameters after oral administration of GDC-0980 (0.
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CAS 1032754-93-0 Apitolisib

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