NT157 |
Catalog No.GC12712
One-Click Copy Product Info
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NT157 is a selective inhibitor of insulin receptor substrate-1/-2 (IRS-1/2).
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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NT157 is a selective inhibitor of insulin receptor substrate-1/-2 (IRS-1/2)[1]. IRS-1/2 are important cytoplasmic adaptor proteins that mediate insulin and insulin-like growth factor 1 (IGF-1) signaling, playing critical roles in glucose metabolism, cell growth, and development[2]. NT157 exerts its effects by inducing apoptosis and disrupting key signaling pathways and is commonly used in drug research and development for various diseases, including melanoma, prostate cancer, and colorectal cancer[3,4].
In vitro, pretreatment of osteosarcoma MG-63 and U-2OS cells with NT157 (3μM) for 24h significantly inhibited cell migration ability, accompanied by downregulation of IRS-2 protein[5]. Treatment of H1299 and H460 cells with NT157 (3.2, 6.4, 12.5μM) for 7 days resulted in a dose-dependent and significant inhibition of colony formation ability; at the concentration of 12.5μM, the colony formation rates of H1299 and H460 cells decreased to 1.4% and 0.8% of the control group, respectively[6].
In vivo, NT157 (100mg/kg; twice daily) was administered via intraperitoneal injection for 4 weeks in a nude mouse model of lung metastasis of hepatocellular carcinoma established by tail vein injection of SMMC-7721 cells, significantly reducing the incidence of lung metastasis compared to the control group[7]. NT157 (70mg/kg; thrice weekly) was administered via intravenous injection for 4 weeks in mice subcutaneously inoculated with A375SM cells, 48h after the final dose, pY(705)Stat3 levels in tumor tissues were significantly reduced[4].
References:
[1] DE QUEIROZ G N, LIMA K, DE MIRANDA L B L, et al. NT157 exhibits antineoplastic effects by targeting IRS and STAT3/5 signaling in multiple myeloma[J]. Hematology, Transfusion and Cell Therapy, 2024, 46: S112-S121.
[2] RABIEE A, KRÜGER M, ARDENKJÆR-LARSEN J, et al. Distinct signalling properties of insulin receptor substrate (IRS)-1 and IRS-2 in mediating insulin/IGF-1 action[J]. Cellular Signalling, 2018, 47: 1-15.
[3] IBUKI N, GHAFFARI M, REUVENI H, et al. The tyrphostin NT157 suppresses insulin receptor substrates and augments therapeutic response of prostate cancer[J]. Molecular Cancer Therapeutics, 2014, 13(12): 2827-2839.
[4] FLASHNER-ABRAMSON E, KLEIN S, MULLIN G, et al. Targeting melanoma with NT157 by blocking Stat3 and IGF1R signaling[J]. Oncogene, 2016, 35(20): 2675-2680.
[5] GAROFALO C, CAPRISTO M, MANCARELLA C, et al. Preclinical effectiveness of selective inhibitor of IRS-1/2 NT157 in osteosarcoma cell lines[J]. Frontiers in Endocrinology, 2015, 6: 74.
[6] DE MIRANDA L B L, LIMA K, COELHO-SILVA J L, et al. NT157 exerts antineoplastic activity by targeting JNK and AXL signaling in lung cancer cells[J]. Scientific Reports, 2022, 12(1): 17092.
[7] YU S Z, WANG Y, LV K J, et al. NT157 inhibits HCC migration via downregulating the STAT3/Jab1 signaling pathway[J]. Technology in Cancer Research & Treatment, 2021, 20: 15330338211027916.
| Cell experiment [1]: | |
Cell lines | H1299 and H460 cells |
Preparation Method | H1299 and H460 cells were seeded at a density of 1×103 cells per well in 6-well plates and incubated for 24h, then treated with NT157 (3.2, 6.4, and 12.5μM) for 7 days. Colonies were fixed and stained with 1% crystal violet solution, and the number of colonies was counted to assess clonogenic capacity. |
Reaction Conditions | 3.2, 6.4, and 12.5μM; 7 days |
Applications | Treatment with NT157 significantly inhibited colony formation in a dose-dependent manner, reducing the colony formation rates of H1299 and H460 cells to 1.4% and 0.8% of the control group, respectively, at a concentration of 12.5μM. |
| Animal experiment [2]: | |
Animal models | Mice carrying A375SM xenograft tumors |
Preparation Method | A375SM cells were injected subcutaneously into mice, and administration of NT157 (70mg/kg) by intravenous injection was initiated 10 days later, thrice weekly for 4 weeks. Samples for immunohistochemistry were taken 48h following the last treatment. |
Dosage form | 70mg/kg; thrice weekly; 4 weeks; i.v. |
Applications | Treatment with NT157 significantly reduced the level of pY(705)Stat3 in tumor tissue. |
References: | |
| 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 | 485.1 μL | 2.4257 mL | 4.8513 mL |
| 10 mM | 242.6 μL | 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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)