CAS No. : 1032754-93-0

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000195
Molecular Formula:C₂₃H₃₀N₈O₃S
Molecular Weight:498.6
IC50:5 nM/27 nM/7 nM/14 nM(PI3Kα/β/δ/γ); 17 nM (Ki, mTOR)
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Appearance:white solid powder
Purity: > 98%
Cat No:I000195
Cas No:1032754-93-0

GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively; also a mTOR inhibitor with Ki of 17 nM, and highly selective versus others PIKK family kinases. 

in vitro: GDC-0980 shows the potent and selective inhibitory activities against class I PI3K and mTOR kinase versus a large panel of kinases with Ki of 17 nM for mTOR and IC50 of 5 nM, 27 nM, 7 nM, and 14 nM for PI3Kα, β, δ, and γ, respectively [1]. GDC-0980 reduces cancer cell viability by inhibiting cell-cycle procession and inducing apoptosis with most potency in prostate (IC50 < 200 nM 50%), <500 nM 100%), breast (IC50 <200 nM 37%, <500 nM 78%) and NSCLC lines (IC50 <200 nM 29%, <500 nM 88%) and less potency in pancreatic (IC50 <200 nM 13%, <500 nM 67%) and melanoma cell lines (IC50 <200 nM 0%, <500 nM 33%) [2]. 

in vivo: In both PC-3 and MCF-7 neo/HER2 xenograft models, GDC-0980 at a dose of 1 mg/kg, exhibits significant antitumor activity by causing tumor growth delay. Furthermore, GDC-0980 results in tumor stasis or regressions at the maximum tolerated dose of 7.5 mg/kg [1].

1:A multicenter, single-arm, open-label, phase 2 study of apitolisib (GDC-0980) for the treatment of recurrent or persistent endometrial carcinoma (MAGGIE study). Makker V, Recio FO, Ma L, Matulonis UA, Lauchle JO, Parmar H, Gilbert HN, Ware JA, Zhu R, Lu S, Huw LY, Wang Y, Koeppen H, Spoerke JM, Lackner MR, Aghajanian CA.Cancer. 2016 Sep 7. doi: 10.1002/cncr.30286. [Epub ahead of print] PMID: 27603005
2:Randomized Open-Label Phase II Trial of Apitolisib (GDC-0980), a Novel Inhibitor of the PI3K/Mammalian Target of Rapamycin Pathway, Versus Everolimus in Patients With Metastatic Renal Cell Carcinoma. Powles T, Lackner MR, Oudard S, Escudier B, Ralph C, Brown JE, Hawkins RE, Castellano D, Rini BI, Staehler MD, Ravaud A, Lin W, O/'Keeffe B, Wang Y, Lu S, Spoerke JM, Huw LY, Byrtek M, Zhu R, Ware JA, Motzer RJ.J Clin Oncol. 2016 May 10;34(14):1660-8. doi: 10.1200/JCO.2015.64.8808. Epub 2016 Mar 7. PMID: 26951309
3: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 SO, Wagner AJ, Bendell JC, Kindler HL, Krug LM, Seiwert TY, Zauderer MG, Lolkema MP, Apt D, Yeh RF, Fredrickson JO, Spoerke JM, Koeppen H, Ware JA, Lauchle JO, Burris HA 3rd, de Bono JS.Clin Cancer Res. 2016 Jun 15;22(12):2874-84. doi: 10.1158/1078-0432.CCR-15-2225. Epub 2016 Jan 19. PMID: 26787751 Free PMC Article
4: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 X, Salphati L, Kim A, Morinello E, Wong L, Pang J, Percey S, Meng M, Reuschel S, Dean B.Biomed Chromatogr. 2015 Aug;29(8):1274-9. doi: 10.1002/bmc.3417. Epub 2015 Feb 10. PMID: 25677784
5:GDC-0980-induced apoptosis is enhanced by autophagy inhibition in human pancreatic cancer cells. Tang JY, Dai T, Zhang H, Xiong WJ, Xu MZ, Wang XJ, Tang QH, Chen B, Xu M.Biochem Biophys Res Commun. 2014 Oct 24;453(3):533-8. doi: 10.1016/j.bbrc.2014.09.115. Epub 2014 Oct 5. PMID: 25285629
6: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 X, Li F, McKnight J, Schmidt C, Strooisma K, Shimizu H, Faber K, Ware JA, Dean B.J Pharm Biomed Anal. 2014 Nov;100:150-6. doi: 10.1016/j.jpba.2014.08.001. Epub 2014 Aug 10. PMID: 25165011
7:Oncogenic PIK3CA gene mutations and HER2/neu gene amplifications determine the sensitivity of uterine serous carcinoma cell lines to GDC-0980, a selective inhibitor of Class I PI3 kinase and mTOR kinase (TORC1/2). English DP, Bellone S, Cocco E, Bortolomai I, Pecorelli S, Lopez S, Silasi DA, Schwartz PE, Rutherford T, Santin AD.Am J Obstet Gynecol. 2013 Nov;209(5):465.e1-9. doi: 10.1016/j.ajog.2013.07.020. Epub 2013 Jul 24. PMID: 23891627
8:Preclinical assessment of the absorption and disposition of the phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor GDC-0980 and prediction of its pharmacokinetics and efficacy in human. Salphati L, Pang J, Plise EG, Lee LB, Olivero AG, Prior WW, Sampath D, Wong S, Zhang X.Drug Metab Dispos. 2012 Sep;40(9):1785-96. doi: 10.1124/dmd.112.046052. Epub 2012 Jun 13. PMID: 22696419 Free Article
9:GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Wallin JJ, Edgar KA, Guan J, Berry M, Prior WW, Lee L, Lesnick JD, Lewis C, Nonomiya J, Pang J, Salphati L, Olivero AG, Sutherlin DP, O/'Brien C, Spoerke JM, Patel S, Lensun L, Kassees R, Ross L, Lackner MR, Sampath D, Belvin M, Friedman LS.Mol Cancer Ther. 2011 Dec;10(12):2426-36. doi: 10.1158/1535-7163.MCT-11-0446. Epub 2011 Oct 13. PMID: 21998291 Free Article
10:Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. Sutherlin DP, Bao L, Berry M, Castanedo G, Chuckowree I, Dotson J, Folks A, Friedman L, Goldsmith R, Gunzner J, Heffron T, Lesnick J, Lewis C, Mathieu S, Murray J, Nonomiya J, Pang J, Pegg N, Prior WW, Rouge L, Salphati L, Sampath D, Tian Q, Tsui V, Wan NC, Wang S, Wei B, Wiesmann C, Wu P, Zhu BY, Olivero A.J Med Chem. 2011 Nov 10;54(21):7579-87. doi: 10.1021/jm2009327. Epub 2011 Oct 7. PMID: 21981714
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