1. Protein Tyrosine Kinase/RTK
  2. IGF-1R
  3. GSK1904529A

GSK1904529A 

Cat. No.: HY-10524 Purity: 99.22%
Handling Instructions

GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.

For research use only. We do not sell to patients.

GSK1904529A Chemical Structure

GSK1904529A Chemical Structure

CAS No. : 1089283-49-7

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1  mL in DMSO USD 127 In-stock
Estimated Time of Arrival: December 31
10 mg USD 135 In-stock
Estimated Time of Arrival: December 31
50 mg USD 345 In-stock
Estimated Time of Arrival: December 31
100 mg USD 625 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GSK1904529A purchased from MCE. Usage Cited in: Clin Cancer Res. 2014 Nov 1;20(21):5483-95.

    Effects of GSK1904529A as single agents, respectively, on mediators of IGF-1R- and ERK1/ERK2-signaling pathways.(A-B) Effect of GSK1904529A on phosphorylation of IGF-1R (A) and Erk1/Erk2 (B).
    • Biological Activity

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    • Customer Review

    Description

    GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc. IC50 value: 27/25 nM (IGF1R/IR) [1] Target: IGF1R/IR in vitro: GSK1904529A is a reversible, ATP-competitive inhibitor and has enzyme-inhibitor binding values against IGF-1R and IR with Ki of 1.6 nM and 1.3 nM, respectively. GSK1904529A potently inhibits the ligand-induced phosphorylation of IGF-1R and IR at concentrations above 0.01 μM, followed by blocking downstream signaling (AKT, IRS-1, and ERK). GSK1904529A potently inhibits NIH-3T3/LISN, TC-71, SK-N-MC, SK-ES RD-ES cells with IC50 of 60 nM, 35 nM, 43 nM, 61 nM and 62 nM, respectively. GSK1904529A also inhibits other multiple myeloma and Ewing's sarcoma cell lines including NCI-H929, MOLP-8, LP-1 and KMS-12-BM etc. GSK1904529A induces cell cycle arrest at the G1 phase in cell lines COLO 205, MCF-7, and NCI-H929, which are sensitive to GK1904529A [1]. in vivo: GSK1904529A indicates 98% tumor growth inhibition in NIH-3T3/LISN tumor-bearing mice at a dose of 30 mg/kg (orally, twice-daily) and 75% in COLO 205 xenografts mice (once daily). Among HT29 and BxPC3 xenografts, GSK1904529A produces moderate tumor growth inhibition with no side effects at a dose of 30 mg/kg. Meanwhile, GSK1904529A shows minimal effects on blood glucose levels. GSK1904529A (~3.5 μM in blood) completely inhibits IGF-1R phosphorylation. GSK1904529A has been implicated in treatment of various IGF-1R-dependent tumors including prostate, colon, breast, pancreatic, ovarian, and sarcomas [1].

    Molecular Weight

    851.96

    Formula

    C₄₄H₄₇F₂N₉O₅S

    CAS No.

    1089283-49-7

    SMILES

    O=C(C1=CC(C2=C(N3C=CC=CC3=N2)C4=NC(NC5=CC(CC)=C(C=C5OC)N6CCC(CC6)N7CCN(CC7)S(=O)(C)=O)=NC=C4)=CC=C1OC)NC8=C(C=CC=C8F)F

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (58.69 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.1738 mL 5.8688 mL 11.7376 mL
    5 mM 0.2348 mL 1.1738 mL 2.3475 mL
    10 mM 0.1174 mL 0.5869 mL 1.1738 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.75 mg/mL (3.23 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    GSK1904529AIGF-1RInsulin-like growth factor-1 receptorInhibitorinhibitorinhibit

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