| Identification | Back Directory | [Name]
GSK1904529A | [CAS]
1089283-49-7 | [Synonyms]
CS-29
GSK 4529
GSK1904529A
GSK1904529A, >=98%
IGF-IR, IGF-IIR inhibitor
GSK1904529A ISO 9001：2015 REACH
GSK1904529A;GSK-1904529A;GSK 1904529A
GSK1904529A : IGF-IR, IGF-IIR inhibitor
N-(2,6-Difluorophenyl)-5-[3-[2-[[5-ethyl-2-(methyloxy)-4-[4-[4-(methylsulfonyl)-1-piperazinyl]
N-(2,6-difluorophenyl)-5-(3-(2-(5-ethyl-2-methoxy-4-(4-(4-(methylsulfonyl)piperazin-1-yl)piperidin-1-yl)phenylamino)pyrimidin-4-yl)H-imidazo[1,2-a]pyridin-2-yl)-2-methoxybenzamide
Benzamide, 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-
N-(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
N-(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 GSK 1904529A | [Molecular Formula]
C44H47F2N9O5S | [MDL Number]
MFCD17010271 | [MOL File]
1089283-49-7.mol | [Molecular Weight]
851.96 |
| Chemical Properties | Back Directory | [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 | [InChIKey]
MOSKATHMXWSZTQ-UHFFFAOYSA-N | [SMILES]
C(NC1=C(F)C=CC=C1F)(=O)C1=CC(C2=C(C3C=CN=C(NC4=CC(CC)=C(N5CCC(N6CCN(S(C)(=O)=O)CC6)CC5)C=C4OC)N=3)N3C(=N2)C=CC=C3)=CC=C1OC |
| Hazard Information | Back Directory | [Uses]
A selective inhibitor of IGF-1R and IR with IC50s of 27 nM and 25 nM, respectively. | [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. | [in vivo]
GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has antitumor activity in mice[1].
GSK1904529A (1-30 mg/kg; a single p.o.) decreases IGF-I-induced IGF-IR phosphorylation in a dose-dependent manner in mice[1].
GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has no significant alterations in the blood glucose levels in mice[1]. | Animal Model: | Female athymic nu/nu CD-1 mice are bring NIH-3T3/LISN tumor[1] | | Dosage: | 30 mg/kg | | Administration: | P.o. once or twice daily for 21 d | | Result: | Resulted in 56% (once daily) and 98% (twice daily) inhibition of tumor growth.
No significant decrease in body weight on the once-daily schedule.
Observed 11-13% of body weight loss, and recovered to near baseline 6 days after the cessation of treatment in twice-daily group.
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| [target]
IGF1R | [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. |
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