NCI677397
Based on 1 publication(s) in Google Scholar
NCI677397 is a USP24 inhibitor. NCI677397 increases lipid ROS, activates cholesterol and fatty acid biosynthesis, degrades ABC transporters, GPX4 and DHFR through the autophagy pathway, decreases the level of P-gp and ultimately leads to ferroptosis in drug-resistant cancer cells. NCI677397 can be used for the study of lung caner and brain cancer.
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- CAS 番号: 907547-06-2
- 分子式: C28H31N3OS
- 分子量:457.63
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 NCI677397
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生物活性
製品説明
IC50 & Target
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GPX4 |
体外実験
NCI677397 (0-120 nM, 24 h-7 d) effectively reverses drug resistance in multiple cancer types: Lung cancer (T24 cells) resistant to Taxol, Brain cancer (Pt3-TMZR and U87-R cells) resistant to TMZ (HY-17364), Nasopharyngeal cancer (Hone-1-CPTR cells) resistant to CPT (HY-16560) and Colorectal cancer (HCT116-OXR cells) resistant to Oxaliplatin (HY-17371)[2].
NCI677397 (10 and 20 μM, 4 days) significantly reduces the viability of TMZ-sensitive and -resistant GBM cells and there is a synergistic effect combined with TMZ[1].
NCI677397 (0-20 μM, 24 h) induces autophagy, not apoptosis in both TMZ-sensitive and TMZ-resistant GBM cells and A549 and Taxol-resistant A549 (A549-T24) cells[1].
NCI677397 (0-15 μM, 24 h) induces the biosynthesis of cholesterol and fatty acid in U87, U87R, Pt’3, Pt’3R, A549 and A549-T24 cells[1].
NCI677397 (0-25 μM, 24 h) induces ferroptosis mediated via lipid ROS in U87, U87R, Pt’3, Pt’3R and A549-T24 cells[1].
NCI677397 (0-25 μM, 24 h) degrades ABCG1/5/8 through the autophagy pathway and reduces the stability of GPX4 and DHFR in Pt’3R and A549-T24 cells[1].
NCI677397 (20 μM, 0-24 h) induces lipid peroxidation within 2 hours, upregulates cholesterol synthase 6 hours later, and completes the ferroptosis process 24 hours later in Pt’3R cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TMZ-sensitive GBM cells (Pt’3, A172 and U87 cells) and TMZ-resistant GBM cells (Pt’3R, A172R and U87R cells)
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Concentration:0, 10 and 20 μM
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Incubation Time:4 days
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Result:Significantly decreased the viability combined with TMZ treatment.
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Cell Line:TMZ-sensitive GBM cells (Pt’3, A172 and U87 cells) and TMZ-resistant GBM cells (Pt’3R, A172R and U87R cells)
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Concentration:0, 5, 10, 15, 20 μM
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Incubation Time:24 h
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Result:Increased the levels of autophagosome-associated lipidated form of LC3B (LC3B-II).
Did not increase the levels of Bax, an apoptotic marker.
Increased autophagic and apoptotic cell death with TMZ.
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Cell Line:Pt’3R cells
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Concentration:15 μM
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Incubation Time:24 h
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Result:Induced accumulation of LC3B spots.
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Cell Line:Pt’3, Pt’3R and A549-T24cells
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Concentration:0, 5, 10, 15, 20, 25 μM
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Incubation Time:24 h
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Result:Increased the levels of p-IRE1a, Bip, XBP1, p-eIF2a and CHOP in Pt’3 cells.
Increased the levels of ACSL3 and ACSL4 in brain and lung cancer cells.
Increased heme oxygenase-1 (HO-1) and p62/SQSTM1.
Induced SLC47A1 upregulation in both A549-T24 and Pt30R cells.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:U87R xenograft model established in male nonobese diabetic/severe combined immunodeficiency mice (8 weeks old)[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection (i.p.), twice a week for 7 weeks
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Result:Led to smaller tumor size and lowered tumor weight.
化学情報
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CAS 番号 907547-06-2
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分子量 457.63
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分子式 C28H31N3OS
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SMILES
O=C(C1=CC=C2SC3=C(N(CCCCN4CCN(CC4)C)C2=C1)C=CC=C3)C5=CC=CC=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Poult Sci
Ferroptosis bridges early-life oxidative stress and lifetime meat quality defects in broilers. [Abstract]2026 May 15;105(8):107133. PMID: 42184739
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (218.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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: ≥ 5 mg/mL (10.93 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.93 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
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.
純度とドキュメンテーション
参考文献
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1852 mL | 10.9259 mL | 21.8517 mL | 54.6293 mL |
| 5 mM | 0.4370 mL | 2.1852 mL | 4.3703 mL | 10.9259 mL | |
| 10 mM | 0.2185 mL | 1.0926 mL | 2.1852 mL | 5.4629 mL | |
| 15 mM | 0.1457 mL | 0.7284 mL | 1.4568 mL | 3.6420 mL | |
| 20 mM | 0.1093 mL | 0.5463 mL | 1.0926 mL | 2.7315 mL | |
| 25 mM | 0.0874 mL | 0.4370 mL | 0.8741 mL | 2.1852 mL | |
| 30 mM | 0.0728 mL | 0.3642 mL | 0.7284 mL | 1.8210 mL | |
| 40 mM | 0.0546 mL | 0.2731 mL | 0.5463 mL | 1.3657 mL | |
| 50 mM | 0.0437 mL | 0.2185 mL | 0.4370 mL | 1.0926 mL | |
| 60 mM | 0.0364 mL | 0.1821 mL | 0.3642 mL | 0.9105 mL | |
| 80 mM | 0.0273 mL | 0.1366 mL | 0.2731 mL | 0.6829 mL | |
| 100 mM | 0.0219 mL | 0.1093 mL | 0.2185 mL | 0.5463 mL |
NCI677397 関連分類
HY-176557 関連分類
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