NVP-AEW541
Based on 13 publication(s) in Google Scholar
NVP-AEW541 (AEW541 ) is an orally active inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with an IC50 value of 0.15 μM. NVP-AEW541 also inhibits InsR, IC50 with a value of 0.14 μM. NVP-AEW541 has antitumor activity.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.92%
- CAS 番号: 475489-16-8
- 分子式: C27H29N5O
- 分子量:439.55
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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溶剤 & 溶解度
- プロトコル
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MedChemExpress（MCE）の使用を引用している文献 NVP-AEW541
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Adv Sci (Weinh). 2026 Mar 12:e20455. [Abstract]
- Phytomedicine. 2025 Oct 5:148:157378. [Abstract]
- NPJ Parkinsons Dis. 2025 Jun 7;11(1):157. [Abstract]
- Cell Rep. 2025 Mar 11;44(3):115381. [Abstract]
- Life Sci. 2025 Feb 5:123449. [Abstract]
- ACS Chem Neurosci. 2021 Aug 4;12(15):2917-2928. [Abstract]
- Endocr Relat Cancer. 2019 Feb;26(2):187-199. [Abstract]
- Stem Cells Int. 2021 Dec 6:2021:5553676. [Abstract]
- PLoS One. 2018 Feb 7;13(2):e0192214. [Abstract]
- J Hand Surg Am. 2025 Apr 14:S0363-5023(25)00132-7. [Abstract]
- Anticancer Drugs. 2024 Jan 1;35(1):46-54. [Abstract]
- bioRxiv. 2025 Nov 14.
生物活性
IC50: 0.15 ±0.036 μM (IGF-IR), 0.14±0.039 μM (InsR), 0.42±0.11 μM (Flt-3), 2±0.61 μM (PDGFR), 2.4±0.38 μM (c-Src), 3.3±1.4 μM (c-Kit)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
20 nM
Compound: NVP-AEW541
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Inhibition of full length IGF-1 receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation
Inhibition of full length IGF-1 receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation
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[PMID: 26951753] |
| BaF3 | IC50 |
244 nM
Compound: NVP-AEW541
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Inhibition of full length insulin receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation
Inhibition of full length insulin receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation
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[PMID: 26951753] |
| HEK293 | IC50 |
0.13 μM
Compound: NVP-AEW541
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Displacement of [3H]-dofetilide from human ERG channel expressed in HEK293 cells
Displacement of [3H]-dofetilide from human ERG channel expressed in HEK293 cells
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[PMID: 26951753] |
| HEK293 | IC50 |
65 nM
Compound: NVP-AEW541
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Inhibition of full length IGF-1 receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis
Inhibition of full length IGF-1 receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis
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[PMID: 26951753] |
| HEK293 | IC50 |
892 nM
Compound: NVP-AEW541
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Inhibition of full length insulin receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis
Inhibition of full length insulin receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis
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[PMID: 26951753] |
| Sf21 | IC50 |
2300 nM
Compound: 21; NVP-AEW541
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Inhibition of human recombinant 1R N-terminal His-tagged (919 to 1343 residues) expressed in baculovirus infected Sf21 measured after 20 mins by western blot analysis
Inhibition of human recombinant 1R N-terminal His-tagged (919 to 1343 residues) expressed in baculovirus infected Sf21 measured after 20 mins by western blot analysis
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[PMID: 36324498] |
| Sf21 | IC50 |
86 nM
Compound: 21; NVP-AEW541
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Inhibition of human recombinant IGF-1R N-terminal His-tagged (950 to 1337 residues) expressed in baculovirus infected Sf21 measured after 20 mins by western blot analysis
Inhibition of human recombinant IGF-1R N-terminal His-tagged (950 to 1337 residues) expressed in baculovirus infected Sf21 measured after 20 mins by western blot analysis
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[PMID: 36324498] |
NVP-AEW541 inhibits the in vitro kinase activity of the recombinant IGF-IR kinase domain with an IC50 value of 0.15 μM and to be equipotent against the recombinant InsR kinase domain. NVP-AEW541 is confirmed active toward the IGF-IR kinase (IC50=86 nM) and shown to be selective at the cellular level. Indeed, NVP-AEW541 is found to be 27-fold more potent toward the native IGF-IR, as compared to the structurally related native InsR (IC50=2.3 μM). NVP-AEW541 suppresses the IGF-I-mediated survival, soft agar and proliferation of MCF-7 cells with IC50 of 0.162 μM, 0.105 μM and 1.64 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 475489-16-8
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性状 Solid
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分子量 439.55
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分子式 C27H29N5O
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Color White to light yellow
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SMILES
NC1=C2C(N([C@@H]3C[C@@H](C3)CN4CCC4)C=C2C5=CC=CC(OCC6=CC=CC=C6)=C5)=NC=N1
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別名
AEW541
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Adv Sci (Weinh)
IGFBP5 Restores Endometrial Receptivity and Rescues Implantation Failure in Polycystic Ovary Syndrome. [Abstract]2026 Mar 12:e20455. PMID: 41816941 -
Phytomedicine
Cistanche deserticola extract and its active components, echinacoside, ameliorate sarcopenia by activating the IGF-1/PI3K-AKT pathway to modulate ferroptosis. [Abstract]2025 Oct 5:148:157378. PMID: 41106096 -
NPJ Parkinsons Dis
2025 Jun 7;11(1):157. PMID: 40483356 -
Cell Rep
YAP1 is a key regulator of EWS::FLI1-dependent malignant transformation upon IGF-1-mediated reprogramming of bone mesenchymal stem cells. [Abstract]2025 Mar 11;44(3):115381. PMID: 40080499 -
Life Sci
2025 Feb 5:123449. PMID: 39920984 -
ACS Chem Neurosci
Abnormal Insulin-like Growth Factor 1 Signaling Regulates Neuropathic Pain by Mediating the Mechanistic Target of Rapamycin-Related Autophagy and Neuroinflammation in Mice. [Abstract]2021 Aug 4;12(15):2917-2928. PMID: 34264648 -
Endocr Relat Cancer
2019 Feb;26(2):187-199. PMID: 30422809 -
Stem Cells Int
Mechanical Stress-Induced IGF-1 Facilitates col-I and col-III Synthesis via the IGF-1R/AKT/mTORC1 Signaling Pathway. [Abstract]2021 Dec 6:2021:5553676. PMID: 34912459 -
PLoS One
Extraocular muscle regeneration in zebrafish requires late signals from Insulin-like growth factors. [Abstract]2018 Feb 7;13(2):e0192214. PMID: 29415074 -
J Hand Surg Am
2025 Apr 14:S0363-5023(25)00132-7. PMID: 40232216 -
Anticancer Drugs
2024 Jan 1;35(1):46-54. PMID: 37449977 -
溶剤 & 溶解度
DMSO : 50 mg/mL (113.75 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 2.5 mg/mL (5.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (5.69 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (25.0 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.
プロトコル
The activities of protein kinases are assayed in the presence or absence of inhibitors by measuring the incorporation of 33P from [γ33P]ATP (1000 Ci/mmol) into appropriate substrates. The protein kinase assays are carried out in 96-well plates at RT under conditions described in details below andterminated by the addition of 20 μL of 125 mM EDTA. Subsequently, 30 μL (c-Abl, c-Src, IGF-1R) or 40 μL (all other kinases) of the reaction mixture are transferred onto Immobilon-PVDF pre-soaked for 5 min with methanol, rinsed with water, then soaked for 5 min with 0.5 % H3PO4 and mounted on vacuum manifold. After spotting all samples, vacuum is connected and each well rinsed with 200 μL 0.5 % H3PO4. Membranes are removed and washed 4× on a shaker with 1% H3PO4, once with ethanol. After drying, mounting in Packard TopCount 96- well frame, and adding of 10 μL/well of Microscint, membranes are counted. IC50 values are calculated by linear regression analysis of the percentage inhibition of each compound in duplicate, at four concentrations (usually 0.01, 0.1, 1, and 10 μM).One unit of protein kinase activity is defined as 1 nmole of 33P transferred from [γ33P]ATP to the substrate protein per minute per mg of protein at 37C[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Between 3000 and 6000 cells/well are seeded in 96-well plates with a total media volume of 100 μL/well. Increasing concentrations of the compound are added 24 hr thereafter in quadruplicate. 72 hr later, cells are fixed by addition of 25 μL/well Glutaraldehyde (20%) and incubation for 10 min at RT. Cells are then washed 2× with 200μL/well H2O and 100μL Methylene Blue (0.05%) is added. After incubation for 10 min at RT, cells are washed 3× with 200 μL/well H2O. 200 μL/well HCl (3%) is added, and following incubation for 30 min at RT on a plate shaker, absorbance is measured at 650 nm[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Female Harlan athymic nude mice are used NWT-21 cells are grown in DMEM (high glucose, 4.5 g/L), 10% FCS, 1% L-glutamine, and 1% Na-pyruvate. 5×106 cells/animal are initially injected s.c. into the right flank of five mice. For the in vivo efficacy experiment, tumors of 500 to 800 mm3 are excised and nonnecrotic areas are cut to fragments of 3×3×3 mm. Tumor fragments are washed in sterile PBS and one tumor fragment per animal is trans- planted s.c. into the right flank. Tumor volumes (length×width ×height×π/6) and body weights are determined three times weekly. At the first day of treatment (day 0), the therapy group (NVP-AEW541) and the control group (vehicle only) are selected by stratification (8 animals per group, average tumor volume of about 95 mm3 per group). Animals are treated p.o. twice daily, 7 days/week either with NVP-AEW541 (20, 30, or 50 mg/kg; 10 mL/kg dissolved in 25 mM L(+)-tartaric acid, therapy group) or with 25 mM L(+)-tartaric acid (control group). Antitumor activity is expressed as T/C%(mean increase of tumor volumes of treated animals divided by the mean increase of tumor volumes of control animals multiplied by 100). The experiment is terminated when the mean tumor volume is about 1500 mm3.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (288 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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取扱説明書 (2659 KB)
参考文献
[1]. García-Echeverría C, et al. In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell. 2004 Mar;5(3):231-9. [Content Brief]
[2]. Tanno B, et al. Down-regulation of IGF-1 receptor activity by NVP-AEW541 has an antitumor effect on neuroblastoma cells in vitro and in vivo. Clin Cancer Res. 2006, 12(22), 6772-6780. [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 | 2.2751 mL | 11.3753 mL | 22.7505 mL | 56.8764 mL |
| 5 mM | 0.4550 mL | 2.2751 mL | 4.5501 mL | 11.3753 mL | |
| 10 mM | 0.2275 mL | 1.1375 mL | 2.2751 mL | 5.6876 mL | |
| 15 mM | 0.1517 mL | 0.7584 mL | 1.5167 mL | 3.7918 mL | |
| 20 mM | 0.1138 mL | 0.5688 mL | 1.1375 mL | 2.8438 mL | |
| 25 mM | 0.0910 mL | 0.4550 mL | 0.9100 mL | 2.2751 mL | |
| 30 mM | 0.0758 mL | 0.3792 mL | 0.7584 mL | 1.8959 mL | |
| 40 mM | 0.0569 mL | 0.2844 mL | 0.5688 mL | 1.4219 mL | |
| 50 mM | 0.0455 mL | 0.2275 mL | 0.4550 mL | 1.1375 mL | |
| 60 mM | 0.0379 mL | 0.1896 mL | 0.3792 mL | 0.9479 mL | |
| 80 mM | 0.0284 mL | 0.1422 mL | 0.2844 mL | 0.7110 mL | |
| 100 mM | 0.0228 mL | 0.1138 mL | 0.2275 mL | 0.5688 mL |
NVP-AEW541 関連分類
HY-50866 関連分類
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