A dual InsR and IGF-1R kinase inhibitor (IC50s = 25 and 27 nM

GSK1904529A – 1 mg

Brand:
Cayman
CAS:
1089283-49-7
Storage:
-20
UN-No:
Non-Hazardous - /

GSK1904529A is a dual inhibitor of the insulin receptor (InsR) and insulin-like growth factor 1 receptor (IGF-1R) kinases (IC50s = 25 and 27 nM, respectively, in a cell-free assay).{48691} It selectively inhibits InsR and IGF-1R kinases over a panel of 45 serine/threonine and tyrosine kinases (IC50s = >1 µM for all). GSK1904529A decreases proliferation of 13 cancer cell lines, including multiple myeloma, sarcoma, colon, and breast cancer cells, with IC50 values ranging from 35 to 189 nM in a panel of 35 cell lines. It reduces tumor growth in NIH3T3-LISN, COLO 205, HT-29, and BxPC3 mouse xenograft models when administered at a dose of 30 mg/kg for 21 days.  

 

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SKU: 29155 - 1 mg Category:

Description

A dual InsR and IGF-1R kinase inhibitor (IC50s = 25 and 27 nM, respectively, in a cell-free assay); selectively inhibits InsR and IGF-1R kinases over a panel of 45 serine/threonine and tyrosine kinases (IC50s = >1 µM for all); decreases proliferation of 13 cancer cell lines including multiple myeloma, sarcoma, colon, and breast cancer cells (IC50s = 35-189 nM) in a panel of 35 cell lines; reduces tumor growth in NIH3T3-LISN, COLO 205, HT-29, and BxPC3 mouse xenograft models at 30 mg/kg for 21 days

Formal name: N-(2,6-difluorophenyl)-5-[3-[2-[[5-ethyl-2-methoxy-4-[4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl]phenyl]amino]-4-pyrimidinyl]imidazo[1,2-a]pyridin-2-yl]-2-methoxy-benzamide

Synonyms: 

Molecular weight: 852

CAS: 1089283-49-7

Purity: ≥95%

Formulation: A solid

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