A dual PI3K and mTOR inhibitor (EC50s = 4

NVP-BGT226 – 5 mg

Brand:
Cayman
CAS:
1245537-68-1
Storage:
-20
UN-No:
- /

NVP-BGT226 is an orally bioavailable dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR).{35140} It inhibits class I PI3Ks with EC50 values of 4, 63, and 38 nM for PI3Kα, β, and γ isoforms, respectively, in a filter binding assay. It binds to both class I and class III PI3Ks in a quantitative ELISA assay with EC50 values of 55.8 and 7.03 nM, for HsPI3Kβ and HsVps34, respectively.{35142} It decreases protein levels of phosphorylated mTOR and Akt, a downstream target of PI3K signaling.{36351} NVP-BGT226 inhibits the growth of squamous cell carcinoma cell lines, HONE-1, and a variant of HONE-1 resistant to cisplatin (Item No. 13119) with IC50 values of 7.4-27.8, 22.6, and 30.1 nM, respectively.{35138} It halts the cell cycle at the G0/G1 phase and induces autophagy. NVP-BGT226 (2.5 and 5 mg/kg daily for three weeks) inhibits tumor growth in a FaDu head and neck cancer mouse xenograft model.  

 

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Description

A dual PI3K and mTOR inhibitor (EC50s = 4, 63, and 38 nM for PI3Kα, β, and γ isoforms, respectively, in a filter binding assay); binds to class I and class III PI3Ks (EC50s = 55.8 and 7.03 nM, for HsPI3Kβ and HsVps34, respectively); decreases protein levels of phosphorylated mTOR and Akt; inhibits the growth of squamous cell carcinoma cell lines, HONE-1, and a variant of HONE-1 resistant to cisplatin (IC50s = 7.4-27.8, 22.6, and 30.1 nM, respectively); inhibits tumor growth in a FaDu mouse xenograft model at doses of 2.5 and 5 mg/kg daily for three weeks

Formal name: 1,3-dihydro-8-(6-methoxy-3-pyridinyl)-3-methyl-1-[4-(1-piperazinyl)-3-(trifluoromethyl)phenyl]-2H-imidazo[4,5-c]quinolin-2-one, (2Z)-2-butenedioate

Synonyms: 

Molecular weight: 650.6

CAS: 1245537-68-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Autophagy||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cancer|Multidrug Resistance||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|Autophagy

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