NVP-ADW742
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.30%
- No. CAS: 475488-23-4
- Fòrmula: C28H31N5O
- Peso molecular:453.58
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) NVP-ADW742
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Actividad biológica
IC50: 0.17 μM (IGF-1R) and 2.8 μM (InsR)[1]
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Cell Line
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Type | Value | Description | References |
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| HeLa | IC50 |
3.05 μM
Compound: NVP-ADW742
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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
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[PMID: 29624387] |
| Sf21 | IC50 |
78 nM
Compound: 1
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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
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[PMID: 17689078] |
| Vero C1008 | IC50 |
1 μM
Compound: NVP-ADW742
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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
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[PMID: 29624387] |
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.
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Cell Line:A panel of cell lines from multiple myeloma (MM), other hematologic malignancies and solid tumors
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Concentration:0.1, 0.5, 1, 2, 5, 10 µM
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Incubation Time:72 hours
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Result:Dose-dependently inhibited serum-induced cell growth in all cell lines.
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Cell Line:NWT-21 cells
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Concentration:0.1, 0.3, 1, 3, 9 µM
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Incubation Time:20 min
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Result:Blocked IGF-1-induced phosphorylation of IGF-1R and its known downstream target Akt at submicromolar concentrations.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6- to 8-week-old male SCID/NOD mice with diffuse skeletal lesions of luciferase-expressing MM cells[1]
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Dosage:10 mg/kg (IP) or 50 mg/kg (orally)
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Administration:IP or orally; twice daily for 19 days
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Result:Significantly suppressed tumor growth and prolonged the survival of mice.
Chemical Information
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No. CAS 475488-23-4
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Appearance Solid
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Peso molecular 453.58
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Fòrmula C28H31N5O
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Color White to light yellow
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SMILES
NC1=C2C(N(C=C2C3=CC=CC(OCC4=CC=CC=C4)=C3)[C@H]5C[C@@H](C5)CN6CCCC6)=NC=N1
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Synonyms
ADW742; GSK 552602A; ADW
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Blood
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.
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Theranostics
LXR activation potentiates sorafenib sensitivity in HCC by activating microRNA-378a transcription. [Abstract]2020 Jul 11;10(19):8834-8850. PMID: 32754282 -
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (285 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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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