A dual inhibitor of PI3K and mTOR (Kiapps = 2

GDC-0084 – 1 mg

Brand:
Cayman
CAS:
1382979-44-3
Storage:
-20
UN-No:
Non-Hazardous - /

GDC-0084 is a dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR) with Kiapp values of 2, 46, 3, 10, and 70 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, and mTOR, respectively.{45137} It inhibits the proliferation of PC3 cells in vitro (EC50 = 0.4 μM). GDC-0084 (25 mg/kg) reduces phosphorylation of Akt in mouse brain. It reduces tumor growth in a U87 MG/M human glioblastoma mouse xenograft model when administered at doses greater than 2.2 mg/kg and induces tumor regression when administered at a dose of 17.9 mg/kg. GDC-0084 (25 and 50 mg/kg) also reduces tumor growth in an A431 cutaneous squamous cell carcinoma (cSCC) mouse xenograft model.{45138}  

 

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SKU: 26390 - 1 mg Category:

Description

A dual inhibitor of PI3K and mTOR (Kiapps = 2, 46, 3, 10, and 70 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, and mTOR, respectively); inhibits the proliferation of PC3 cells in vitro (EC50 = 0.4 μM); reduces phosphorylation of Akt in mouse brain at 25 mg/kg; reduces tumor growth in a U87 MG/M human glioblastoma mouse xenograft model at >2.2 mg/kg and induces tumor regression at 17.9 mg/kg; reduces tumor growth in an A431 cSCC mouse xenograft model at 25 and 50 mg/kg

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

Synonyms: 

Molecular weight: 382.4

CAS: 1382979-44-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|mTOR||Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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