GSK1904529A


CAS No. : 1089283-49-7

1089283-49-7
Price and Availability of CAS No. : 1089283-49-7
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10mg $149 In-stock
50mg $380 In-stock
100mg $688 In-stock
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Cat. No. : HY-10524
M.Wt: 851.96
Formula: C44H47F2N9O5S
Purity: >98 %
Solubility: DMSO : 50 mg/mL (58.69 mM; Need ultrasonic)
Introduction of 1089283-49-7 :

GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity[1][2]. IC50 & Target: IC50: 27 nM (IGF-1R), 25 nM (IR)[1] In Vitro: GSK1904529A displays high affinities for IGF-1R and IR, with Kis of 1.6 and 1.3 nM, respectively[1].
GSK1904529A (72 h) inhibits tumor cells proliferation with IC50s ranges from 35 nM to >30 μM, and Ewing's sarcoma and multiple myeloma cell lines are greatest sensitive[1].
GSK1904529A (0.03-3 μM; 24 and 48 h) arrests cells at the G1 phase of the cell cycle[1].
GSK1904529A (2 h) inhibits phosphorylation of IGF-IR and IR with IC50s of 22 and 19 nM in NIH-3T3/LISN and NIH-3T3-hIR cells, respectively[1].
GSK1904529A (0.01-3 μM; 4 h) blocks the major downstream signal transduction pathways mediated by IGF-IR and IR in NIH-3T3/LISN and NIH-3T3-hIR cells[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].

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