GDC-0084( RG-7666 )

Catalog No. M11585 CAS No. 1382979-44-3

COA

Datasheet

HNMR

HPLC

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Product Name

GDC-0084
Note

Research use only, not for human use.
Brief Description

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.
Description

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; highly selective against a panel of 229 kinases (IC50>1 uM); shows antiproliferative (EC50 =0.3-1.1 uM) in 5 GBM cell lines; significantly and dose-dependently inhibits tumor growth in a subcutaneous U87 tumor xenograft model of glioblastoma in mice.Brain Cancer Phase 2 Discontinued.
In Vitro

——
In Vivo

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Synonyms

RG-7666
Pathway

Cancer
Target

Brain Cancer
Recptor

mTOR|PI3Kα|PI3Kβ|PI3Kγ|PI3Kδ
Research Area

Cancer
Indication

Brain Cancer

CAS Number

1382979-44-3
Formula Weight

382.4197
Molecular Formula

C18H22N8O2
Purity

>98% (HPLC)
Solubility

DMSO: 6 mg/mL (Need ultrasonic)
SMILES

NC1=NC=C(C2=NC(N3CCOCC3)=C4N=C(C(C)(C)OCC5)N5C4=N2)C=N1
Chemical Name

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

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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