2. Protein Tyrosine Kinase/RTK
    Apoptosis
  3. IGF-1R
    Insulin Receptor
    Apoptosis
  4. GSK1904529A

GSK1904529A 

Cat. No.: HY-10524 Purity: 99.66%
COA Handling Instructions

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.

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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10 mM * 1 mL in DMSO USD 140 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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50 mg USD 380 In-stock
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100 mg USD 688 In-stock
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Customer Review

Based on 6 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.  [Abstract]

    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

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Cycle Analysis[1]

    Cell Line: COLO 205, MCF-7, and NCI-H929 cells
    Concentration: 0, 0.03, 0.1, 0.3, 1, 3 μM
    Incubation Time: 24 and 48 hours
    Result: Increased the accumulation in G1 and decreased accumulation in S and G2-M phases of the cell cycle.

    Western Blot Analysis[1]

    Cell Line: NIH-3T3/LISN and NIH-3T3-hIR cells
    Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 μM
    Incubation Time: 4 hours
    Result: Inhibited the ligand-induced phosphorylation of IGF-IR and IR at concentrations >0.01 μM.
    Decreased the phosphorylation of AKT, IRS-1, and ERK.
    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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.
    Molecular Weight

    851.96

    Appearance

    Solid

    Formula

    C44H47F2N9O5S
    CAS No.
    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)

    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 available by MCE.
    Purity & Documentation
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    GSK1904529A1089283-49-7IGF-1RInsulin ReceptorApoptosisInsulin-like growth factor-1 receptorinsulinIRanti-tumorInhibitorinhibitorinhibit

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