Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.

NVP-AEW541 [475489-16-8]

Imprimer

Référence HY-50866-5mg

Conditionnement : 5mg

Marque : MedChemExpress

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Description

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^[1].

IC₅₀ & Target

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]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	20 nM Compound: NVP-AEW541	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	[PMID: 26951753]
BaF3	IC₅₀	244 nM Compound: NVP-AEW541	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	[PMID: 26951753]
HEK293	IC₅₀	0.13 μM Compound: NVP-AEW541	Displacement of [3H]-dofetilide from human ERG channel expressed in HEK293 cells Displacement of [3H]-dofetilide from human ERG channel expressed in HEK293 cells	[PMID: 26951753]
HEK293	IC₅₀	65 nM Compound: NVP-AEW541	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	[PMID: 26951753]
HEK293	IC₅₀	892 nM Compound: NVP-AEW541	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	[PMID: 26951753]
Sf21	IC₅₀	2300 nM Compound: 21; NVP-AEW541	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	[PMID: 36324498]
Sf21	IC₅₀	86 nM Compound: 21; NVP-AEW541	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	[PMID: 36324498]

In Vitro

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.

Solvant et solubilité

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2751 mL	11.3753 mL	22.7505 mL
5 mM	0.4550 mL	2.2751 mL	4.5501 mL
10 mM	0.2275 mL	1.1375 mL	2.2751 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.

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: ≥ 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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation

Purity: 99.92%

Fiche technique (288 KB) SDS (393 KB)

COA (259 KB) LCMS (94 KB)

Instruction de manipulation (2659 KB)

Références

[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]

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Référence HY-50866-5mg

Marque : MedChemExpress

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