Login / Register
0

GSK1904529A

GSK1904529A

Catalog Number:
L002368295APE
Mfr. No.:
APE-A1302
Price:
$450
  • Size:
    Quantity:
    Add to Cart:
    Add to Cart
      • Overview

        • Please contact us at for specific academic pricing.

          Background

          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.

          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
        • Alternative Name
          N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonylpiperazin-1-yl)piperidin-1-yl]anilino]pyrimidin-4-yl]imidazo[1,2-a]pyridin-2-yl]-2-methoxybenzamide
          CAS Number
          1089283-49-7
          Molecular Formula
          C44H47F2N9O5S
          Molecular Weight
          851.96
          Appearance
          A solid
          Purity
          98.17%
          Solubility
          ≥42.6 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
          Storage
          Store at -20°C

          * For Research Use Only

    We Also Recommend

    Gatifloxacin

    Gatifloxacin

    Gatifloxacin

    Gatifloxacin

    $167

    Mosapride Citrate

    Mosapride Citrate

    $229

    Mosapride Citrate

    Mosapride Citrate

    $228

    Note: If you don't receive our verification email, do the following:

    Products
    Amerigo Scientific
    Support
    Contact Us
    Copyright © Amerigo Scientific. All rights reserved.