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

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.

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GSK1904529A Chemical Structure

GSK1904529A Chemical Structure

CAS No. : 1089283-49-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 140 In-stock
Solution
10 mM * 1 mL in DMSO USD 140 In-stock
Solid
1 mg USD 38 In-stock
5 mg USD 96 In-stock
10 mg USD 149 In-stock
50 mg USD 380 In-stock
100 mg USD 688 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

GSK1904529A Related Antibodies

Top Publications Citing Use of Products

    GSK1904529A purchased from MedChemExpress. 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).

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    • Purity & Documentation

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    • 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].

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

    GSK1904529A Related Antibodies

    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].

    MedChemExpress (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

    Formula

    C44H47F2N9O5S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (58.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.1738 mL 5.8688 mL 11.7376 mL 29.3441 mL
    5 mM 0.2348 mL 1.1738 mL 2.3475 mL 5.8688 mL
    10 mM 0.1174 mL 0.5869 mL 1.1738 mL 2.9344 mL
    15 mM 0.0783 mL 0.3913 mL 0.7825 mL 1.9563 mL
    20 mM 0.0587 mL 0.2934 mL 0.5869 mL 1.4672 mL
    25 mM 0.0470 mL 0.2348 mL 0.4695 mL 1.1738 mL
    30 mM 0.0391 mL 0.1956 mL 0.3913 mL 0.9781 mL
    40 mM 0.0293 mL 0.1467 mL 0.2934 mL 0.7336 mL
    50 mM 0.0235 mL 0.1174 mL 0.2348 mL 0.5869 mL
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    GSK1904529A Related Classifications

    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.

    Keywords:

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

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