A dual inhibitor of PI3K and mTOR (IC50s = 3.4

GNE-493 – 25 mg

Brand:
Cayman
CAS:
1033735-94-2
Storage:
-20
UN-No:
Non-Hazardous - /

GNE-493 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC50s = 3.4, 12, 16, 16, and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, and mTOR, respectively).{24603} It inhibits proliferation of PC3 and MCF-7.1 cells with IC50 values of 330 and 180 nM, respectively. GNE-493 (10 mg/kg per day) reduces tumor volume in PC3 and MCF-7.1 mouse xenograft models, which are PTEN negative or PI3Kα activating mutation positive, respectively. It also decreases relative levels of phosphorylated Akt, PRAS40, and S6RP in tumor tissue in the MCF-7.1 mouse xenograft model.  

 

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SKU: 29224 - 25 mg Category:

Description

A dual inhibitor of PI3K and mTOR (IC50s = 3.4, 12, 16, and 16 nM for PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively); inhibits proliferation of PC3 and MCF-7.1 cells (IC50s = 330 and 180 nM, respectively); reduces tumor volume in PC3 and MCF-7.1 mouse xenograft models at 10 mg/kg per day

Formal name: 2-(2-amino-5-pyrimidinyl)-α,α-dimethyl-4-(4-morpholinyl)-thieno[3,2-d]pyrimidine-6-methanol

Synonyms: 

Molecular weight: 372.4

CAS: 1033735-94-2

Purity: ≥98%

Formulation: A crystalline solid

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