A selective inhibitor of PI3Kα (Ki = 0.2 nM); is 133-

GDC-0326 – 25 mg

Brand:
Cayman
CAS:
1282514-88-8
Storage:
-20
UN-No:
Non-Hazardous - /

GDC-0326 is an inhibitor of phosphatidylinositol 3-kinase α (PI3Kα; Ki = 0.2 nM) that is 133-, 20-, and 51-fold selective for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively.{43203} It inhibits proliferation of MCF7-neo/HER2 and PC3 cells (EC50s = 0.1 and 2.2 μM, respectively). In vivo, GDC-0326 (6.25 mg/kg) induces tumor regression in a KPL-4 mouse xenograft model. It also reduces tumor growth, tumor vasculature, and the number of liver and lymph node metastases in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors.{43204}  

 

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Description

A selective inhibitor of PI3Kα (Ki = 0.2 nM); is 133-, 20-, and 51-fold selective for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively; inhibits proliferation of MCF7-neo/HER2 and PC3 cells (EC50s = 0.1 and 2.2 μM, respectively); induces tumor regression in a KPL-4 mouse xenograft model at 6.25 mg/kg; reduces tumor growth, tumor vasculature, and the number of liver and lymph node metastases in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors

Formal name: (2S)-2-[[5,6-dihydro-2-[1-(1-methylethyl)-1H-1,2,4-triazol-5-yl]imidazo[1,2-d][1,4]benzoxazepin-9-yl]oxy]-propanamide

Synonyms: 

Molecular weight: 382.4

CAS: 1282514-88-8

Purity: ≥98%

Formulation: A crystalline solid

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

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