For research use only. Not for therapeutic Use.
GDC-0084（Cat No.:I001476）is an experimental small molecule inhibitor that targets the phosphoinositide 3-kinase (PI3K)/Akt/mTOR signaling pathway, which plays a critical role in cell growth, survival, and metabolism. It has shown promise in preclinical studies as a potential treatment for various cancers, particularly those with alterations in this pathway, such as glioblastoma and breast cancer. GDC-0084 selectively inhibits the class I PI3K isoform, helping to reduce tumor cell proliferation and survival. Ongoing clinical trials are evaluating its safety, pharmacokinetics, and efficacy as a cancer therapy, though more data is needed for approval.
| Catalog Number | I001476 |
| CAS Number | 1382979-44-3 |
| Synonyms | 5-(6,6-dimethyl-4-morpholino-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl)pyrimidin-2-amine |
| Molecular Formula | C₁₈H₂₂N₈O₂ |
| Purity | ≥95% |
| Target | PI3K |
| Solubility | DMSO: ≥ 6 mg/mL |
| Storage | Store at -20C |
| IUPAC Name | 5-(6,6-dimethyl-4-morpholin-4-yl-8,9-dihydropurino[8,9-c][1,4]oxazin-2-yl)pyrimidin-2-amine |
| InChI | InChI=1S/C18H22N8O2/c1-18(2)16-22-12-14(25-3-6-27-7-4-25)23-13(11-9-20-17(19)21-10-11)24-15(12)26(16)5-8-28-18/h9-10H,3-8H2,1-2H3,(H2,19,20,21) |
| InChIKey | LGWACEZVCMBSKW-UHFFFAOYSA-N |
| SMILES | CC1(C2=NC3=C(N2CCO1)N=C(N=C3N4CCOCC4)C5=CN=C(N=C5)N)C |
| Reference | </br>1:Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma. Salphati L, Alicke B, Heffron TP, Shahidi-Latham S, Nishimura M, Cao T, Carano RA, Cheong J, Greve J, Koeppen H, Lau S, Lee LB, Nannini-Pepe M, Pang J, Plise EG, Quiason C, Rangell L, Zhang X, Gould SE, Phillips HS, Olivero AG.Drug Metab Dispos. 2016 Dec;44(12):1881-1889. Epub 2016 Sep 16. PMID: 27638506 </br>2:Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR. Heffron TP, Ndubaku CO, Salphati L, Alicke B, Cheong J, Drobnick J, Edgar K, Gould SE, Lee LB, Lesnick JD, Lewis C, Nonomiya J, Pang J, Plise EG, Sideris S, Wallin J, Wang L, Zhang X, Olivero AG.ACS Med Chem Lett. 2016 Feb 16;7(4):351-6. doi: 10.1021/acsmedchemlett.6b00005. eCollection 2016 Apr 14. PMID: 27096040 Free PMC Article |
