NT157 |
| Catalog No.GC12712 |
IRS-1/2 inhibitor, inhibits IGF-1R and STAT3 signaling pathway
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1384426-12-3
Sample solution is provided at 25 µL, 10mM.
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IC50: 0.3 to 0.8 μM
NT157 is an IRS-1/2 inhibitor.
Insulin receptor substrates 1 and 2 (IRS1/2) mediate antiapoptotic and mitogenic signaling from insulin receptor (IR), insulin-like growth factor 1 receptor (IGF-IR), and other oncoproteins. IRS1 plays a critical role in cancer cell proliferation, and its expression is increased in many human malignancies.
In vitro: NT157 treatment was fonund to be able to lead to dose-dependent suppression of IRS protein expression, inhibition of IGF1R activation, inhibition of IGF1-induced AKT activation, but increased ERK activation in NT157-treated cells. These effects were associated with decreased proliferation, increased apoptosis of LNCaP cells and increased G2-M arrest in PC3 cells. Moreover, NT157 could significantly affect the cell migratory ability, as demonstrated by a wound-healing assay. In addition, the NT157 treatment was able to induce cell cycle arrest and inhibit IGF system signaling [1].
In vivo: In previous animal study, NT157 was found to suppress androgen-responsive growth, delay CRPC progression of LNCaP xenografts, and suppress PC3 tumor growth alone or in combination with docetaxel. This study reported the first preclinical proof-of-principle data that NT157 suppressed IRS1/2 expression, delayed CRPC progression, and suppressed growth of CRPC tumors in vivo [1].
Clinical trial: Up to now, NT157 is still in the preclinical development stage.
Reference:
[1] Ibuki N et al. The tyrphostin NT157 suppresses insulin receptor substrates and augments therapeutic response of prostate cancer. Mol Cancer Ther. 2014 Dec;13(12):2827-39.
| Cas No. | 1384426-12-3 | SDF | |
| Chemical Name | (E)-3-(3-bromo-4,5-dihydroxyphenyl)-N-(3,4,5-trihydroxybenzyl)prop-2-enethioamide | ||
| Canonical SMILES | OC1=C(O)C=C(/C=C/C(NCC2=CC(O)=C(O)C(O)=C2)=S)C=C1Br | ||
| Formula | C16H14BrNO5S | M.Wt | 412.26 |
| Solubility | ≥ 50mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4257 mL | 12.1283 mL | 24.2565 mL |
| 5 mM | 0.4851 mL | 2.4257 mL | 4.8513 mL |
| 10 mM | 0.2426 mL | 1.2128 mL | 2.4257 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.)
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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