GDC-0084

• CAT Number: I001476
• CAS Number: 1382979-44-3
• Molecular Formula: C₁₈H₂₂N₈O₂
• Molecular Weight: 382.42
• Purity: ≥95%
• Synonyms: 5-(6,6-dimethyl-4-morpholino-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl)pyrimidin-2-amine
• Target: PI3K
• Solubility: DMSO: ≥ 6 mg/mL
• Storage: Store at -20C
• 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

GDC-0084 is a potent, selective inhibitor of Class I PI3K and mTOR with good penetration across the blood-brain barrier.[1] [2]

Reference

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 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