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GDC-0980

GDC-0980 is an inhibitor of PI3K and mTORC1/2 that exhibits anticancer chemotherapeutic and anti-angiogenic activities. GDC-0980 inhibits cell growth in uterine serous carcinoma cells and decreases vascular density by altering vascular permeability parameter K (trans) in other cellular models. GDC-0980 inhibits cell growth and tumor growth across many cancer cell lines and models, including breast cancer, prostate cancer, and lung cancer.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18926327

Cas No.

1032754-93-0

Purity

≥98%

Formula

C23H30N8O3S

Formula Wt.

498.60

IUPAC Name

(2S)-1-[4-[[2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one

Synonym

RG7422

Appearance

White to off white powder

English DP, Bellone S, Cocco E, et al. 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). Am J Obstet Gynecol. 2013 Nov;209(5):465.e1-9. PMID: 23891627.

Sampath D, Oeh J, Wyatt SK, et al. Multimodal microvascular imaging reveals that selective inhibition of class I PI3K is sufficient to induce an antivascular response. Neoplasia. 2013 Jul;15(7):694-711. PMID: 23814482.

Wallin JJ, Edgar KA, Guan J, et al. GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther. 2011 Dec;10(12):2426-36. PMID: 21998291.

MK 8931