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NT157 IGF-1R inhibitor

Name: NT157
Brand: Selleck Chemicals
SKU: S8228
Rating: 5 (16 reviews)

Cat.No.S8228

NT157, a selective inhibitor of IRS-1/2 (insulin receptor substrate), has the potential to inhibit IGF-1R and STAT3 signalling pathways in cancer cells and stroma cells of TME leading to a decrease in cancer cell survival.

Chemical Structure

Molecular Weight: 412.26

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Quality Control

Batch: Purity: 98.91%

98.91

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2
Other IGF-1R Inhibitors	Linsitinib (OSI-906) BMS-536924 NVP-AEW541 BMS-754807 Picropodophyllin (AXL1717) GSK1904529A AG-1024 NVP-ADW742 PQ 401 MSDC-0160

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description	PMID
KB-8-5-11	qHTS assay	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen, Potency = 7.3078 μM.	31515284
KB-3-1	qHTS assay	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	31515284
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	412.26	Formula	C₁₆H₁₄BrNO₅S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1384426-12-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=C(C=C(C(=C1O)O)O)CNC(=S)C=CC2=CC(=C(C(=C2)Br)O)O

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (198.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 82 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (24.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	IRS1/2
In vitro	NT157 treatment resulted in dose-dependent inhibition of IGF1R activation, suppression of IRS protein expression, inhibition of IGF1-induced AKT activation, but increased ERK activation in this compound-treated cells in vitro. These effects were correlated with decreased proliferation and increasing apoptosis of LNCaP cells and increasing G2-M arrest in PC3 cells. This chemical can mediate suppression of IGF1R-mediated survival signalling through the established mechanism for negative feedback of IGF1R signalling: targeting IRS1/2 for serine phosphorylation and subsequent degradation. It displayed little to no effect on the survival of normal melanocytes and fibroblasts.
In vivo	NT157 suppressed androgen-responsive growth, delayed CRPC progression of LNCaP xenografts, and suppressed PC3 tumour growth alone and in combination. Melanoma tumour growth and metastasis is efficiently inhibited by this compound.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25267499/ [2] https://pubmed.ncbi.nlm.nih.gov/23651636/

Applications

Methods	Biomarkers	Images	PMID
Western blot	IRS-1 / IRS-2 p-IRS1 / p-AKT / AKT / p-S6 / S6 / Shc / p-ERK / ERK		26029165
Growth inhibition assay	Cell viability		26029165

Tech Support

Handling Instructions

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