A PI3Kα inhibitor (IC50 = 6.8 nM); selective for PI3Kα over PI3Kβ

CNX-1351 – 25 mg

Brand:
Cayman
CAS:
1276105-89-5
Storage:
-20
UN-No:
Non-Hazardous - /

CNX-1351 is a covalent inhibitor of PI3Kα (IC50 = 6.8 nM).{56002} It is selective for PI3Kα over PI3Kβ, -γ, and -δ (IC50s = 166, 240.3, and 3,020 nM, respectively), as well as PI3KC2A, PI3KC, PI4Kα, PI4Kβ, SPHK1, and SPHK2 (IC50s = >1 µM for all). CNX-1351 (500 nM) inhibits phosphorylation of Akt in SKOV3 cells. It inhibits the growth of SKOV3 and MCF-7 cancer cells (GI50s = 77.6 and 54.7 nM, respectively). CNX-1351 (100 mg/kg) inhibits Akt phosphorylation in mouse spleen.  

 

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SKU: 30264 - 25 mg Category:

Description

A PI3Kα inhibitor (IC50 = 6.8 nM); selective for PI3Kα over PI3Kβ, -γ, and -δ (IC50s = 166, 240.3, and 3,020 nM, respectively), as well as PI3KC2A, PI3KC, PI4Kα, PI4Kβ, SPHK1, and SPHK2 (IC50s = >1 µM for all); inhibits phosphorylation of Akt in SKOV3 cells at 500 nM; inhibits the growth of SKOV3 and MCF-7 cancer cells (GI50s = 77.6 and 54.7 nM, respectively); inhibits Akt phosphorylation in mouse spleen at 100 mg/kg

Formal name: 1-[4-[[2-(1H-indazol-4-yl)-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-6-methyl-5-heptene-1,4-dione

Synonyms: 

Molecular weight: 573.7

CAS: 1276105-89-5

Purity: ≥98%

Formulation: A crystalline solid

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