NT157
Based on 2 publication(s) in Google Scholar
NT157 (Tyrphostin NT157) is a selective IRS-1/2 inhibitor that induces Ser-phosphorylation and consequently the degradation of IRS-1/2. NT157 (Tyrphostin NT157) is a first-in-class anti-cancer agent that also targets Stat3 signaling pathway.
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- Purity: 99.38%
- CAS No.: 1384426-12-3
- 화학식: C16H14BrNO5S
- 분자량:412.26
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) NT157
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WB
Biological Activity
NT157 (0.3-3 μM; 72 hours) shows a strong dose-dependent inhibition of growth in all cell lines tested, and the IC50 s ranges from 0.3 to 0.8 μM[1].
NT157 (1-3 μM; 24 hours) induces cell cycle arrest in MG-63 and U-2OS OS cells[1].
NT157 (1-3 μM; 48 hours) downregulates the Tyr-phosphorylation of IRS-1 in the MG-63 and U-2OS cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MG-63, OS-19, and U-2OS cells
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Concentration:0.3, 1, 3 μM
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Incubation Time:72 hours
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Result:Showed a strong dose-dependent inhibition of growth, and the IC50s ranges from 0.3 to 0.8 μM.
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Cell Line:MG-63, U-2OS OS cells
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Concentration:1, 3 μM
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Incubation Time:24 hours
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Result:Induced cell cycle arrest in the G2/M phase.
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Cell Line:MG-63, U-2OS OS cells
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Concentration:1, 3 μM
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Incubation Time:48 hours
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Result:Downregulated the Tyr-phosphorylation of IRS-1 in the MG-63 and U-2OS cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6- to 8- week-old male athymic nude mice (LNCaP xenografts)[3]
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Dosage:50 mg/kg
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Administration:i.p.; three times per week for 6 weeks
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Result:Significantly delayed tumor growth.
Chemical Information
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CAS No. 1384426-12-3
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Appearance Solid
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분자량 412.26
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화학식 C16H14BrNO5S
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Color Light yellow to yellow
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SMILES
S=C(NCC1=CC(O)=C(O)C(O)=C1)/C=C/C2=CC(O)=C(O)C(Br)=C2
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Synonyms
Tyrphostin NT157
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
miR-130a and miR-145 reprogram Gr-1+CD11b+ myeloid cells and inhibit tumor metastasis through improved host immunity. [Abstract]2018 Jul 4;9(1):2611. PMID: 29973593
NT157 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Jul 4;9(1):2611. [Abstract]
Western blot of Gr-1+CD11b+myeloid cells collected from spleen of 4T1 tumor-bearing mice treated with NT157 (n=5).
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Cell Death Dis
Activation of AKT via a dual mechanism enhances the susceptibility of melanoma cells to glucose deprivation. [Abstract]2025 Aug 7;16(1):595. PMID: 40774947
용액&용해도
DMSO : ≥ 30 mg/mL (72.77 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (6.06 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 (6.06 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 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.
순도&문서
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Data Sheet (277 KB)
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SDS (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Downregulated the Tyr-phosphorylation of IRS-1 in the MG-63 and U-2OS cells. [Content Brief]
[2]. Flashner-Abramson E, et al. Targeting melanoma with NT157 by blocking Stat3 and IGF1R signaling. Oncogene. 2016 May 19;35(20):2675-80. [Content Brief]
[3]. 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. [Content Brief]
[4]. Ishii H, et al. miR-130a and miR-145 reprogram Gr-1+CD11b+ myeloid cells and inhibit tumor metastasis through improved host immunity. Nat Commun. 2018 Jul 4;9(1):2611. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4257 mL | 12.1283 mL | 24.2565 mL | 60.6413 mL |
| 5 mM | 0.4851 mL | 2.4257 mL | 4.8513 mL | 12.1283 mL | |
| 10 mM | 0.2426 mL | 1.2128 mL | 2.4257 mL | 6.0641 mL | |
| 15 mM | 0.1617 mL | 0.8086 mL | 1.6171 mL | 4.0428 mL | |
| 20 mM | 0.1213 mL | 0.6064 mL | 1.2128 mL | 3.0321 mL | |
| 25 mM | 0.0970 mL | 0.4851 mL | 0.9703 mL | 2.4257 mL | |
| 30 mM | 0.0809 mL | 0.4043 mL | 0.8086 mL | 2.0214 mL | |
| 40 mM | 0.0606 mL | 0.3032 mL | 0.6064 mL | 1.5160 mL | |
| 50 mM | 0.0485 mL | 0.2426 mL | 0.4851 mL | 1.2128 mL | |
| 60 mM | 0.0404 mL | 0.2021 mL | 0.4043 mL | 1.0107 mL |
NT157 Related Classifications
HY-100037 Related Classifications
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