CH5132799 – 10 mg

Brand:
Cayman
CAS:
1007207-67-1
Storage:
-20
UN-No:
Non-Hazardous - /

CH5132799 is an inhibitor of class I PI3K isoforms (IC50s = 14, 120, 500, and 36 nM for PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively).{42659} It is selective for these PI3K isoforms over PI3KC2α and PI3KC2β, which are class II PI3Ks, Vps34, a class III PI3K, and mTOR (IC50s = 5,300, >10,000, >10,000, and 1,600 nM, respectively), as well as 26 additional protein kinases (IC50s = >10,000 nM). CH5132799 inhibits proliferation of HCT116, KPL-4, T47D, and SKOV3 cancer cells expressing the activating mutation PI3KαH1047R (IC50s = 200, 32, 56, and 120 nM, respectively). It also reduces tumor growth in a PC3 mouse xenograft model when administered at a dose of 25 mg/kg per day.  

 

Available on backorder

SKU: 26410 - 10 mg Category:

Description

An inhibitor of class I PI3K isoforms (IC50s = 14, 120, 500, and 36 nM for PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively); selective for these PI3K isoforms over PI3KC2α, PI3KC2β, Vps34, and mTOR (IC50s = 5,300, >10,000, >10,000, and 1,600 nM, respectively), as well as 26 additional protein kinases (IC50s = >10,000 nM); inhibits proliferation of HCT116, KPL-4, T47D, and SKOV3 cells containing the PI3KαH1047R activating mutation (IC50s = 200, 32, 56, and 120 nM, respectively); reduces tumor growth in a PC3 mouse xenograft model at 25 mg/kg per day


Formal name: 5-[6,7-dihydro-7-(methylsulfonyl)-2-(4-morpholinyl)-5H-pyrrolo[2,3-d]pyrimidin-4-yl]-2-pyrimidinamine

Synonyms: 

Molecular weight: 377.4

CAS: 1007207-67-1

Purity: ≥95%

Formulation: A crystalline solid


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