Cat. No. Name Size Price Add Cart
KI0629Gsk1904529A10 mg$608
Gsk1904529A50 mg$1728
Gsk1904529A200 mg$5248

Chemical Characteristic

Product NameGsk1904529A
CAS No.1089283-49-7
Molecular Weight 851.96
FormulaC44H47F2N9O5S
Chemical NameN-(2,6-Difluorophenyl)-5-[3-[2-[[5-ethyl-2-(methyloxy)-4-[4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl]phenyl]amino]-4-pyrimidinyl]imidazo[1,2-a]pyridin-2-yl]-2-(methyloxy)benzamide
SmilesC(=O)(c1c(ccc(c1)c1nc2ccccn2c1c1nc(ncc1)Nc1c(cc(c(c1)CC)N1CCC(CC1)N1CCN(CC1)S(=O)(=O)C)OC)OC)Nc1c(cccc1F)F
Chemical Structure

Biological activities

GSK1904529A is a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase. GSK1904529A selectively inhibits IGF-IR and IR. The IC50 of GSK1904529A is 27 and 25 nM against IGF-IR and IR, respectively. GSK1904529A blocks receptor autophosphorylation and downstream signaling, leading to cell cycle arrest. GSK1904529A inhibits the proliferation of cell lines derived from solid and hematologic malignancies, with multiple myeloma and Ewing's sarcoma cell lines being most sensitive. Oral administration of GSK1904529A decreases the growth of human tumor xenografts in mice, consistent with a reduction of IGF-IR phosphorylation in tumors. A single oral dose of GSK1904529A given at 1, 3, 10, and 30 mg/kg results in 57%, 75%, 95%, and 99% decrease in IGF-I??nduced IGF-IR phosphorylation, respectively. A single 30 mg/kg dose of GSK1904529A reduces ligand-induced IGF-IR phosphorylation in NIH-3T3-LISN tumor xenografts by >90% 4 to 8 hours after GSK1904529A administration. [1]

Protocols

GSK1904529A is dissolved in DMSO at 10mM. [1]

References

[1] Sabbatini P, et al. Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase. Clin Cancer Res. 2009, 15(9): 3058-3067.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.
KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.