1- (4- ((2- (2- aminopyrimidin- 5- yl)- 7- methyl- 4- morpholinothieno(3,2- d)pyrimidin- 6- yl)methyl)piperazin- 1- yl)- 2- hydroxypropan- 1- one

01/01/2015 - "Here, we investigate the activity of GDC-0980, a novel dual PI3K/mTOR inhibitor, which has been proposed to be effective in mesothelioma. "
01/01/2015 - "In summary, we show that GDC-0980 is effective in mesothelioma 3D models that display ATG13 puncta, and that blockade of autophagy increases their response to chemotherapy. "
01/01/2015 - "We found that a subset of mesothelioma spheroids is sensitive to GDC-0980 alone and to its combination with chemotherapy. "
01/01/2015 - "In this work, we aimed to identify mechanisms and markers of efficacy for GDC-0980 by utilizing 3D models of mesothelioma, both in vitro multicellular spheroids and ex vivo tumor fragment spheroids grown from patient tumor samples. "
01/01/2016 - "Here, we studied the combinatorial therapeutic efficacy of the MET/ALK inhibitor crizotinib, with either a pan-class I PI3K inhibitor, BKM120, or with a PI3K/mTOR dual inhibitor, GDC-0980, in mesothelioma. "

11/01/2013 - "GDC-0980 reduced viable tumor pO2 during a 3-day treatment period, and a significant reduction was also produced by B20.4.1.1. "
01/01/2021 - "Maximum anti-tumor (from tumor growth inhibition to tumor regression) efficiency was observed in all three xenograft models when T-DM1 was combined with GDC-0980. "
01/01/2021 - "Along with its anti-tumor effect, GDC-0980 effectively decreased tumor angiogenesis (CD31 staining). "
01/01/2021 - "A tipping-point for apoptosis following dual inhibition of HER2 signaling network by T-DM1 plus GDC-0980 maximizes anti-tumor efficacy."
01/01/2015 - "In tumor fragment spheroids grown from 21 tumors, we also found a subset (n = 11) that was sensitive to GDC-0980, a sensitivity that also correlated with the presence of ATG13 puncta. "

01/01/2019 - "We set out to evaluate the efficacy of GDC-0980, in pre-clinical studies, against pediatric leukemia cells. "
01/01/2019 - "These findings provide initial proof-of-concept data and rationale for further investigation of GDC-0980 in selected subgroups of pediatric leukemia patients."
01/01/2019 - "Our data show that GDC-0980 significantly inhibited the proliferation of leukemia cell lines, KOPN8 (IC50, 532 nM), SEM (IC50,720 nM), MOLM-13 (IC50,346 nM), MV4;11 (IC50,199 nM), and TIB-202 (IC50, 848 nM), compared to normal control cells (1.23 µM). "
01/01/2019 - "The anti-neoplastic activity of GDC-0980 was evaluated in vitro using five different pediatric leukemia cells. "
01/01/2019 - "Inhibition of PI3K/mTOR Pathways with GDC-0980 in Pediatric Leukemia: Impact on Abnormal FLT-3 Activity and Cooperation with Intracellular Signaling Targets."

10/24/2014 - "Thus, inhibition of autophagy sensitizes GDC-0980-induced anti-pancreatic cancer activity, suggesting a novel therapeutic strategy for GDC-0980 sensitization. "
10/24/2014 - "GDC-0980 inhibited AKT-mTOR activation and pancreatic cancer cell (PANC-1 and Capan-1 lines) survival. "
10/24/2014 - "In the present study, we examined the activity of GDC-0980, a novel class I PI3K/mTOR kinase inhibitor, against pancreatic cancer cells in vitro. "
12/01/2011 - "Correspondingly, GDC-0980 was potent across a broad panel of cancer cell lines, with the greatest potency in breast, prostate, and lung cancers and less activity in melanoma and pancreatic cancers, consistent with KRAS and BRAF acting as resistance markers. "

09/01/2012 - "The objectives of these studies were to characterize the absorption and disposition of GDC-0980 and assess its efficacy in an MCF7-neo/HER2 human breast cancer xenograft model in immunocompromised mice. "