1089283-49-7 Usage
Uses
Different sources of media describe the Uses of 1089283-49-7 differently. You can refer to the following data:
1. A selective inhibitor of IGF-1R and IR with IC50s of 27 nM and 25 nM, respectively.
2. GSK 1904529A is a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 1089283-49-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,8,9,2,8 and 3 respectively; the second part has 2 digits, 4 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1089283-49:
(9*1)+(8*0)+(7*8)+(6*9)+(5*2)+(4*8)+(3*3)+(2*4)+(1*9)=187
187 % 10 = 7
So 1089283-49-7 is a valid CAS Registry Number.
InChI:InChI=1S/C44H47F2N9O5S/c1-5-28-26-35(38(60-3)27-36(28)53-19-15-30(16-20-53)52-21-23-54(24-22-52)61(4,57)58)49-44-47-17-14-34(48-44)42-40(50-39-11-6-7-18-55(39)42)29-12-13-37(59-2)31(25-29)43(56)51-41-32(45)9-8-10-33(41)46/h6-14,17-18,25-27,30H,5,15-16,19-24H2,1-4H3,(H,51,56)(H,47,48,49)
1089283-49-7Relevant articles and documents
Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R)
Emmitte, Kyle A.,Wilson, Brian J.,Baum, Erich W.,Emerson, Holly K.,Kuntz, Kevin W.,Nailor, Kristen E.,Salovich, James M.,Smith, Stephon C.,Cheung, Mui,Gerding, Roseanne M.,Stevens, Kirk L.,Uehling, David E.,Mook Jr., Robert A.,Moorthy, Ganesh S.,Dickerson, Scott H.,Hassell, Anne M.,Anthony Leesnitzer,Shewchuk, Lisa M.,Groy, Arthur,Rowand, Jason L.,Anderson, Kelly,Atkins, Charity L.,Yang, Jingsong,Sabbatini, Peter,Kumar, Rakesh
scheme or table, p. 1004 - 1008 (2009/10/15)
The optimization of imidazo[1,2-a]pyridine inhibitors as potent and selective inhibitors of IGF-1R is presented. Further optimization of oral exposure in mice is also discussed. Detailed selectivity, in vitro activity, and in vivo PK profiles of an optimi