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GDC-0084

Chemical Structure : GDC-0084

CAS No.: 1382979-44-3

GDC-0084 (Paxalisib, RG7666, GDC0084)

Catalog No.: PC-45766Not For Human Use, Lab Use Only.

Paxalisib (GDC-0084, RG7666) is a potent, selective, brain penetrant dual inhibitor of class I PI3Ks and mTOR with Ki of 2/46/3/10/70 nM for PI3Kα/β/δ/γ/mTOR, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Paxalisib (GDC-0084, RG7666) is a potent, selective, brain penetrant dual inhibitor of class I PI3Ks and mTOR with Ki of 2/46/3/10/70 nM for PI3Kα/β/δ/γ/mTOR, respectively.
Paxalisib (GDC-0084, RG7666) is highly selective against a panel of 229 kinases (IC50>1 uM).
Paxalisib (GDC-0084, RG7666) shows antiproliferative (EC50 =0.3-1.1 uM) in 5 GBM cell lines.
Paxalisib (GDC-0084, RG7666) significantly and dose-dependently inhibits tumor growth in a subcutaneous U87 tumor xenograft model of glioblastoma in mice.

Physicochemical Properties

M.Wt 382.4197
Formula C18H22N8O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 6 mg/mL (Need ultrasonic)

Chemical Name/SMILES

2-Pyrimidinamine, 5-[8,9-dihydro-6,6-dimethyl-4-(4-morpholinyl)-6H-[1,4]oxazino[4,3-e]purin-2-yl]-

References

1. Heffron TP, et al. ACS Med Chem Lett. 2016 Feb 16;7(4):351-6.

2. Salphati L, et al. Drug Metab Dispos. 2016 Dec;44(12):1881-1889.

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