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| Cas No.: | 1382979-44-3 |
| Chemical Name: | RG7666; RG-7666; RG 7666; GDC-0084; GDC0084; GDC 0084 |
| Synonyms: | RG7666; RG-7666; RG 7666; GDC-0084; GDC0084; GDC 0084 |
| SMILES: | CC1(C2=NC3=C(N2CCO1)N=C(N=C3N4CCOCC4)C5=CN=C(N=C5)N)C |
| Formula: | C18H22N8O2 |
| M.Wt: | 382.43 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. |
| In Vivo: | After a 25 mg/kg dose of GDC-0084 (Compound 16) administered orally, pAKT in normal mouse brain tissue is significantly inhibited at 1 and 6 h postdose. The potent inhibition of pAKT at both time points in this study demonstrates that GDC-0084 inhibits its target behind a fully intact BBB. In addition to the pharmacodynamic effect in normal brain tissue, GDC-0084 is studied in a subcutaneous U87 tumor xenograft model of glioblastoma in mice. In this study, GDC-0084 achieves significant and dose-dependent tumor growth inhibition. Tumor growth inhibition is first observed at a 2.2 mg/kg dose level. Higher doses led to greater tumor growth inhibition, including tumor regressions at the 17.9 mg/kg dose level. Each of these doses is well tolerated for the duration of the study[1]. |
| In Vitro: | GDC-0084 (Compound 16) maintains inhibition of each of the Class I PI3K isoforms but with more potent inhibition of mTOR. GDC-0084 is also tested in five different GBM cell lines and is found to have antiproliferative EC50s ranging from 0.3 to 1.1 μM[1]. |
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| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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