1. Protein Tyrosine Kinase/RTK Apoptosis
  2. IGF-1R Insulin Receptor Apoptosis
  3. NVP-ADW742

NVP-ADW742  (Synonyms: ADW742; GSK 552602A; ADW)

Cat. No.: HY-10252 Purity: 99.54%
COA Handling Instructions

NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.

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

NVP-ADW742 Chemical Structure

NVP-ADW742 Chemical Structure

CAS No. : 475488-23-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 145 In-stock
Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Solid
1 mg USD 62 In-stock
5 mg USD 132 In-stock
10 mg USD 228 In-stock
50 mg USD 804 In-stock
100 mg USD 1512 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    NVP-ADW742 purchased from MedChemExpress. Usage Cited in: Blood. 2018 Jul 12;132(2):210-222.  [Abstract]

    Phosphorylation of p-ERK1/2 and p-Akt in MKs pretreated with 0.5 μM NVP-ADW742, 10 μM U0126 or 20 μM LY294002 followed by rhIGF-1 treatment for 15 minutes.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells[1][2].

    IC50 & Target

    IC50: 0.17 μM (IGF-1R) and 2.8 μM (InsR)[1]

    In Vitro

    NVP-ADW742 (ADW742; 0.1-10 µM; 72 hours) dose-dependently inhibits serum-induced cell growth in all cell lines[1].
    NVP-ADW742 (0.1-9 µM; 20 min) blocks IGF-1-induced phosphorylation of IGF-1R and its known downstream target Akt at submicromolar concentrations[1].
    NVP-ADW742 has much higher IC50 values for other kinases (IC50>10 μM for HER2, PDGFR, VEGFR-2, or Bcr-Abl p210; and IC50>5 μM for c-Kit)[1].

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

    Cell Viability Assay[1]

    Cell Line: A panel of cell lines from multiple myeloma (MM), other hematologic malignancies and solid tumors
    Concentration: 0.1, 0.5, 1, 2, 5, 10 µM
    Incubation Time: 72 hours
    Result: Dose-dependently inhibited serum-induced cell growth in all cell lines.

    Western Blot Analysis[1]

    Cell Line: NWT-21 cells
    Concentration: 0.1, 0.3, 1, 3, 9 µM
    Incubation Time: 20 min
    Result: Blocked IGF-1-induced phosphorylation of IGF-1R and its known downstream target Akt at submicromolar concentrations.
    In Vivo

    NVP-ADW742 (ADW742; 10 mg/kg for IP or 50 mg/kg for orally; twice daily for 19 days) significantly suppresses tumor growth and prolongs the survival of mice[1].

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

    Animal Model: 6- to 8-week-old male SCID/NOD mice with diffuse skeletal lesions of luciferase-expressing MM cells[1]
    Dosage: 10 mg/kg (IP) or 50 mg/kg (orally)
    Administration: IP or orally; twice daily for 19 days
    Result: Significantly suppressed tumor growth and prolonged the survival of mice.
    Molecular Weight

    453.58

    Formula

    C28H31N5O

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    NC1=C2C(N(C=C2C3=CC=CC(OCC4=CC=CC=C4)=C3)[C@H]5C[C@@H](C5)CN6CCCC6)=NC=N1

    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 : 19.23 mg/mL (42.40 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 2.2047 mL 11.0234 mL 22.0468 mL
    5 mM 0.4409 mL 2.2047 mL 4.4094 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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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: 1.92 mg/mL (4.23 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.92 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (19.2 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 1.92 mg/mL (4.23 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.92 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (19.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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

    Purity: 99.54%

    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 2.2047 mL 11.0234 mL 22.0468 mL 55.1171 mL
    5 mM 0.4409 mL 2.2047 mL 4.4094 mL 11.0234 mL
    10 mM 0.2205 mL 1.1023 mL 2.2047 mL 5.5117 mL
    15 mM 0.1470 mL 0.7349 mL 1.4698 mL 3.6745 mL
    20 mM 0.1102 mL 0.5512 mL 1.1023 mL 2.7559 mL
    25 mM 0.0882 mL 0.4409 mL 0.8819 mL 2.2047 mL
    30 mM 0.0735 mL 0.3674 mL 0.7349 mL 1.8372 mL
    40 mM 0.0551 mL 0.2756 mL 0.5512 mL 1.3779 mL
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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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    Product Name:
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