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: 99.30%
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
10 mM * 1  mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 804 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1512 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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].

    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].

    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.

    475488-23-4

    SMILES

    NC1=C2C(N(C=C2C3=CC=CC(OCC4=CC=CC=C4)=C3)[[email protected]]5C[[email protected]@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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 21.67 mg/mL (47.78 mM; Need ultrasonic)

    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
    10 mM 0.2205 mL 1.1023 mL 2.2047 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: ≥ 2.17 mg/mL (4.78 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.17 mg/mL (4.78 mM); Clear solution

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

    Purity: 99.30%

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    Keywords:

    NVP-ADW742ADW742GSK 552602AADWADW 742ADW-742IGF-1RInsulin ReceptorApoptosisInsulin-like growth factor-1 receptororallyInsRpleiotropicantiproliferativeproapoptotictumormultiplemyelomahematologicmalignanciessolidInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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