5-(6,6-dimethyl-4-morpholino-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl)pyrimidin-2-amine
GDC-0084
CAS: 1382979-44-3
Molecular Formula: C18H22N8O2
5-(6,6-dimethyl-4-morpholino-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl)pyrimidin-2-amine - Names and Identifiers
5-(6,6-dimethyl-4-morpholino-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl)pyrimidin-2-amine - Physico-chemical Properties
| Molecular Formula | C18H22N8O2 |
| Molar Mass | 382.42 |
| Density | 1.60±0.1 g/cm3(Predicted) |
| Solubility | DMSO: 6 mg/mL (Need ultrasonic) |
| pKa | 2.62±0.40(Predicted) |
| Storage Condition | -20℃ |
| Use | Paxalisib (GDC-0084) is a PI3K and mTOR inhibitor that can penetrate the blood-brain barrier. It inhibits PI3Kα,PI3Kβ,PI3Kδ,PI3Kγ and mTOR with Ki values of 2 nM,46 nM,3 nM,10 nM and 70 nM respectively. |
| In vitro study | In microsomal and stem cell cultures, GDC-0084 has good human metabolic stability and can inhibit the key signal pAKT in the PI3K pathway in normal brain tissue. GDC-0084 inhibit the proliferation of a variety of glioma cells, the IC50 range is 0.3-1.1 μm. The binding rate of GDC-0084 to plasma protein is relatively low, and the free fraction in CD-1 mouse plasma is 29.5±2.7(%,n = 3,5 μm), the binding rate to brain tissue was higher in CD-1 mice, with a free fraction of 6.7%(± 1; n = 3). |
| In vivo study | In the mouse brain, GDC-0084 significantly inhibited the PI3K signaling pathway, resulting in up to 90% inhibition of pAkt signaling. GDC-0084 inhibited tumor growth by 70% and 40% in U87 and GS2 orthotopic xenograft models, respectively. Its widespread distribution in brain and intracranial tumors makes it a very effective inhibitor of the PI3K signaling pathway. At present, the efficacy of GDC-0084 is being evaluated in clinical patients, and the tolerated dose of exposure is consistent with the effective dose in mouse models. |
5-(6,6-dimethyl-4-morpholino-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl)pyrimidin-2-amine - Reference
| Reference Show more | 1: 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. Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma. Drug Metab Dispos. 2016 Dec;44(12):1881-1889. Epub 2016 Sep 16. PubMed PMID: 27638506. 2: 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. Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR. ACS Med Chem Lett. 2016 Feb 16;7(4):351-6. doi: 10.1021/acsmedchemlett.6b00005. eCollection 2016 Apr 14. PubMed PMID: 27096040; PubMed Central PMCID: PMC4834666. |
5-(6,6-dimethyl-4-morpholino-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl)pyrimidin-2-amine - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.615 ml | 13.075 ml | 26.149 ml |
| 5 mM | 0.523 ml | 2.615 ml | 5.23 ml |
| 10 mM | 0.261 ml | 1.307 ml | 2.615 ml |
| 5 mM | 0.052 ml | 0.261 ml | 0.523 ml |
Last Update：2024-01-02 23:10:35
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View History
5-(6,6-dimethyl-4-morpholino-8,9-dihydro-6H-[1,4]oxazino[4,3-e]purin-2-yl)pyrimidin-2-amine
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