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%
Handling Instructions Technical Support

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 (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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25 mg In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

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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]

Cellular Effect
Cell Line Type Value Description References
HeLa IC50
3.05 μM
Compound: NVP-ADW742
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
[PMID: 29624387]
Sf21 IC50
78 nM
Compound: 1
Inhibition of human IGF1R expressed in Sf21 cells by time-resolved fluorescence assay
Inhibition of human IGF1R expressed in Sf21 cells by time-resolved fluorescence assay
[PMID: 17689078]
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
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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Volume (final)

V2

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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NVP-ADW742
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