WJ460 |
カタログ番号GC38203
One-Click Copy Product Info
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WJ460は有力なmyoferlin (MYOF)の阻害剤であり、MYOFと直接相互作用できる。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1415251-36-3
Sample solution is provided at 25 µL, 10mM.
WJ460は有力なmyoferlin (MYOF)の阻害剤であり、MYOFと直接相互作用できる[2]。WJ460は乳癌細胞の侵入を遮断し、MDA-MB-231でIC50値は43.37±3.42nMである[2]。しかし、WJ460は代謝安定性、水溶性とMYOFとの結合活性で不足している[3]。
WJ460 (1μM、24時間)はヒトT細胞白血病ウイルスタイプ1（HTLV-1感染）を減らし、これは成体Envの細胞内レベルの減少と関係する[4]。対照群と比べ、WJ460 (50nM 、15時間、2Gy x線)でHCT116（癌細胞株）回転楕円体を処理した結果、接種後の15日目に、成長が減少したため、放射線治療への感受性が明らかに増加した[5].。
WJ460 (10mg/kg；28日間；腹腔内注射)はマウスモデルで、乳癌の成長、血管新生と自発転移を阻害する[2]。WJ460 (10mg/kg；4週間；腹腔内注射)は、フェロプトーシスコア調節因子溶質輸送体ファミリー7メンバー11(SLC7A11)とグルタチオンペルオキシダーゼ 4 (GPX-4)の豊かさを減らした[1]。
WJ460はmyoferlin阻害剤であり、乳癌で抗転移活性を発揮する[2]。
References:
[1] RADEMAKER G, BOUMAHD Y, PEIFFER R, et al. Myoferlin targeting triggers mitophagy and primes ferroptosis in pancreatic cancer cells [J]. Redox Biol, 2022, 53(102324.
[2] ZHANG T, LI J, HE Y, et al. A small molecule targeting myoferlin exerts promising anti-tumor effects on breast cancer [J]. Nat Commun, 2018, 9(1): 3726.
[3] GU H, ZHANG T, LI Y, et al. Discovery of 1,5-diaryl-1,2,4-triazole derivatives as myoferlin inhibitors and their antitumor effects in pancreatic cancer [J]. Future Med Chem, 2022, 14(20): 1425-40.
[4] POLAKOWSKI N, SARKER M A K, HOANG K, et al. HBZ upregulates myoferlin expression to facilitate HTLV-1 infection [J]. PLoS Pathog, 2023, 19(2): e1011202.
[5] FOWLER H, CLIFFORD R E, BOWDEN D, et al. Myoferlin: A Potential Marker of Response to Radiation Therapy and Survival in Locally Advanced Rectal Cancer [J]. Int J Radiat Oncol Biol Phys, 2024, 120(4): 1111-23.
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細胞実験[1]: |
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細胞株 |
膵臓癌細胞株1（PANC-1） |
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準備方法 |
10%のウシ胎児血清(FBS)を添加されたDulbecco's修飾Eagle's培地(DMEM)でPANC-1細胞を維持させた。細胞を37℃、5% CO2のインキュベーターに培養した。細胞を月に一回、マイコプラズマについて検査し、継代1から10まで使った。24時間の間、細胞を50nM WJ460に暴露した。 |
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反応条件 |
50nM；24時間 |
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アプリケーション |
WJ460はG2/M期でマイトファジーと細胞周期停止を惹起する。 |
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動物実験[2]: |
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動物モデル |
雌のヌードマウスBALB/c無胸腺ヌードマウス |
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準備方法 |
自発転移モデルについて、MDA-MB-231-ルシフェラーゼ細胞(1×106)をマウスの#4乳腺脂肪層に注射した。体内画像システムと組織学的な検査で、肺の転移を毎週監視した。 |
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投与形態 |
10mg/kg；28日間；腹腔内注射 |
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アプリケーション |
WJ460は乳癌肺転移を著しく阻害した。 |
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References: [1] RADEMAKER G, BOUMAHD Y, PEIFFER R, et al. Myoferlin targeting triggers mitophagy and primes ferroptosis in pancreatic cancer cells [J]. Redox Biol, 2022, 53(102324. [2] ZHANG T, LI J, HE Y, et al. A small molecule targeting myoferlin exerts promising anti-tumor effects on breast cancer [J]. Nat Commun, 2018, 9(1): 3726. |
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| Cas No. | 1415251-36-3 | SDF | |
| Canonical SMILES | O=C(NCCCCC1=CC=CC=C1)C2=CC=CC(C(N3C4=CC=CC=C4OC)SCC3=O)=C2 | ||
| Formula | C27H28N2O3S | M.Wt | 460.59 |
| 溶解度 | DMSO: 250 mg/mL (542.78 mM) | 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 | 2.1711 mL | 10.8556 mL | 21.7113 mL |
| 5 mM | 434.2 μL | 2.1711 mL | 4.3423 mL |
| 10 mM | 217.1 μL | 1.0856 mL | 2.1711 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 28 reference(s) in Google Scholar.)