Contact us: +91 9550333722 040 - 40102781
Structured search
India
Choose your country
Different countries will display different contents
Try our best to find the right business for you.
My chemicalbook

Welcome back!

HomeProduct name listGSK1904529A

GSK1904529A

GSK1904529A Structural

What is GSK1904529A?

The Uses of GSK1904529A

A selective inhibitor of IGF-1R and IR with IC50s of 27 nM and 25 nM, respectively.

The Uses of GSK1904529A

GSK 1904529A is a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase.

Definition

ChEBI: N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonyl-1-piperazinyl)-1-piperidinyl]anilino]-4-pyrimidinyl]-2-imidazo[1,2-a]pyridinyl]-2-methoxybenzamide is a member of benzamides.

Biological Activity

gsk1904529a is a small-molecule inhibitor of the insulin-like growth factor-i receptor (igf-ir) with ic50 value of 27 nm 1.gsk1904529a is a reversible and atp-competitive inhibitor with ki value of 1.6 nm. in nih-3t3/lisn cells, gsk1904529a potently inhibited phosphorylation of igf-ir with ic50 value of 22 nm. it also demonstrated to be a selective inhibitor since it showed poor inhibitory activity against 45 other serine/threonine and tyrosine kinases. when treated with whole-cell extracts, gsk1904529a significantly inhibited the ligand-induced phosphorylation of igf-ir and decreased phosphorylation of downstream signaling including akt, irs-1 and erk at concentrations > 0.01μm. gsk1904529a suppressed cell proliferation in a variety of tumor cells. the ic50 values for nci-h929, tc-71, sk-n-mc, colo 205, mcf7 and prec are 81, 35, 43, 124, 137 and 68 nm, respectively. in colo 205, mcf-7, and nci-h929 cells, gsk1904529a treatment resulted in cell accumulation in g1 and decrease in s and g2-m phases. moreover, in nih-3t3/lisn xenograft model, once daily administration of gsk1904529a at 30 mg/kg inhibited 56% of tumor growth 1.

References

1. sabbatini p, rowand j l, groy a, et al. antitumor activity of gsk1904529a, a small-molecule inhibitor of the insulin-like growth factor-i receptor tyrosine kinase. clinical cancer research, 2009, 15(9): 3058-3067.

Properties of GSK1904529A

Density  1.39
storage temp.  Store at -20°C
solubility  ≥42.6 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
form  solid
pka 11.12±0.70(Predicted)
color  Light yellow to yellow

Safety information for GSK1904529A

Computed Descriptors for GSK1904529A

Related products of tetrahydrofuran

You may like

Statement: All products displayed on this website are only used for non medical purposes such as industrial applications or scientific research, and cannot be used for clinical diagnosis or treatment of humans or animals. They are not medicinal or edible.