Art. -Nr.: HY-10252

NVP-ADW742

(Synonyms: ADW742; GSK 552602A; ADW)

3 Cited Publications

Kundenbewertung

Based on 3 publication(s) in Google Scholar

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.

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Reinheit: 99.30%
CAS. Nr.: 475488-23-4
Formel: C₂₈H₃₁N₅O
Molecular Weight:453.58

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

NVP-ADW742 Chemical Structure

CAS. Nr.: 475488-23-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]
Vero C1008	IC₅₀	1 μM Compound: NVP-ADW742	Antiviral activity against Ebolavirus Mayinga infected in African green monkey Vero E6 cells after 72 hrs by eGFP assay Antiviral activity against Ebolavirus Mayinga infected in African green monkey Vero E6 cells after 72 hrs by eGFP assay	[PMID: 29624387]

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.

Chemical Information

CAS. Nr. 475488-23-4
Appearance Solid
Molecular Weight 453.58
Formel C₂₈H₃₁N₅O
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
Synonyms

ADW742; GSK 552602A; ADW
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

All WB

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Journal Impact Factor

Blood

IGF-1 facilitates thrombopoiesis primarily through Akt activation. [Abstract]

2018 Jul 12;132(2):210-222. PMID: 29802222

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.
Theranostics

LXR activation potentiates sorafenib sensitivity in HCC by activating microRNA-378a transcription. [Abstract]

2020 Jul 11;10(19):8834-8850. PMID: 32754282
Aquaculture

2025 Aug 15.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.92 mg/mL (4.23 mM); Clear solution

This protocol yields a clear solution of ≥ 1.92 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (19.2 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mitsiades CS, et al. Inhibition of the insulin-like growth factor receptor-1 tyrosine kinase activity as a therapeutic strategy for multiple myeloma, other hematologic malignancies, and solid tumors. Cancer Cell. 2004 Mar;5(3):221-30. [Content Brief]

[2]. Warshamana-Greene GS, et al. The insulin-like growth factor-I (IGF-I) receptor kinase inhibitor NVP-ADW742, in combination with STI571, delineates a spectrum of dependence of small cell lung cancer on IGF-I and stem cell factor signaling. Mol Cancer Ther. 2004 May;3(5):527-35. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

NVP-ADW742

3 Cited Publications

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NVP-ADW742

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) NVP-ADW742

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NVP-ADW742

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) NVP-ADW742

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NVP-ADW742 Related Classifications

HY-10252 Related Classifications