A pan inhibitor of PI3Ks and an inhibitor of mTOR (IC50s = 33

Bimiralisib – 1 mg

Brand:
Cayman
CAS:
1225037-39-7
Storage:
-20
UN-No:
Non-Hazardous - /

Bimiralisib is a potent and orally bioavailable inhibitor of phosphatidylinositol 3-kinases (PI3Ks; IC50s = 33, 661, 708, and 451 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively) and the mammalian target of rapamycin (mTOR; IC50 = 89 nM).{40179} It is selective for these kinases over a panel of cell surface and nuclear receptors, membrane channels, transporters, kinases, proteases, and phosphodiesterases at a concentration of 10 μM. Bimiralisib has anticancer activity with an average GI50 value of 0.7 μM across the National Cancer Institute (NCI) 60 human cancer cell line panel. In vivo, bimiralisib (5-15 mg/kg) reduces tumor growth in a dose-dependent manner in a PC3 prostate cancer mouse xenograft model. Formulations containing bimiralisib are under clinical investigation for the treatment of relapsed and refractory lymphoma and advanced solid tumors.  

 

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SKU: 23441 - 1 mg Category:

Description

A pan inhibitor of PI3Ks and an inhibitor of mTOR (IC50s = 33, 661, 708, 451, and 89 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, and mTOR, respectively); selective for these kinases over a panel of cell surface and nuclear receptors, membrane channels, transporters, kinases, proteases, and phosphodiesterases at a concentration of 10 μM; has anticancer activity (average GI50 = 0.7 μM across the NCI 60 human cancer cell line panel); reduces tumor growth in a dose-dependent manner in a PC3 prostate cancer mouse xenograft model

Formal name: 5-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)-2-pyridinamine

Synonyms:  PI3K-IN-2

Molecular weight: 411.4

CAS: 1225037-39-7

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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