WJ460
目录号 : GC38203
WJ460是一种有效的myoferlin(MYOF)抑制剂,可直接与MYOF相互作用。
Cas No.:1415251-36-3
Sample solution is provided at 25 µL, 10mM.
WJ460 is a potent myoferlin (MYOF) inhibitor, which interacts directly with MYOF[2]. WJ460 blocks breast cancer cell invasion with IC50 values of 43.37±3.42nM in MDA-MB-231[2]. However , WJ460 was inadequate in terms of metabolic stability and water solubility as well as binding activity with MYOF[3].
WJ460 (1μM, 24h) reduced Human T-cell leukemia virus type 1 (HTLV-1 infection) , which was correlated with a reduction in the intracellular level of mature Env[4]. WJ460 (50nM, 15h, 2Gy x-rays) treated HCT116 (cancer cell lines) spheroids were significantly radiosensitized as observed by a reduction in growth at day 15 post-seeding , compared with vehicle cells[5].
WJ460 (10mg/kg; 28 days; intraperitoneal injection) inhibits breast tumor growth, angiogenesis, and spontaneous metastasis in a mouse model[2]. WJ460(10mg/kg; 4weeks; intraperitoneal injection) caused a reduction of the abundance of ferroptosis core regulators solute carrier family 7 member 11 (SLC7A11) and glutathione peroxidase 4 (GPX-4)[1].
WJ460 , a myoferlin inhibitor , exerts anti-metastatic activity in breast cancer[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.
WJ460是一种有效的myoferlin(MYOF)抑制剂,可直接与MYOF相互作用[1]。WJ460阻断乳腺癌细胞侵袭,MDA-MB-231的IC50值为43.37±3.42nM[1]。然而,WJ460在代谢稳定性、水溶性以及与MYOF的结合活性方面存在不足[2]。
WJ460(1μM,24小时)下调了人类T细胞白血病病毒1型(HTLV-1)的感染,这与细胞内成熟Env水平的降低有关[3]。与对照组相比,用WJ460(50nM,15小时,2居里X射线)处理的HCT116(癌细胞系)球体在接种后第15天的生长明显减少,表明其对放射治疗的敏感性增加[4]。
WJ460 (10mg/kg;28天;腹腔注射) 抑制小鼠模型中乳腺肿瘤的生长、血管生成和自发转移[1]。WJ460(10mg/kg ; 4周;腹腔注射)导致铁死亡下调的核心调节因子溶质载体家族7成员11(SLC7A11)和谷胱甘肽过氧化物酶4(GPX-4)丰度降低[5]。
WJ460,作为myoferlin抑制剂,在乳腺癌中有抗转移活性[1]。
Cell experiment[1]: |
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Cell lines |
Pancreatic Cancer Cell Line 1 (PANC-1) |
Preparation method |
PANC-1 cells were maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum (FBS). Cells were cultured in a 37℃, 5% CO2 incubator. Cells were checked monthly for mycoplasma and used between passage 1 and 10. The cells culture were submitted to 50nM WJ460 during 24h. |
Reaction Conditions |
50nM ; 24h |
Applications |
WJ460 triggers a cell cycle arrest in G2/M phase and mitophagy |
Animal experiment[2]: |
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Animal models |
Female nude mice BALB/c athymic nude mice |
Preparation method |
For the spontaneous metastasis model , MDA-MB-231- Luciferase cells (1×106) were injected in the #4 mammary fat pad of the mice. Lung metastasis was monitored weekly by an in vivo image system and histological examination. |
Dosage form |
10mg/kg ; 28 days ; intraperitoneal injection. |
Applications |
WJ460 caused significant inhibition of breast cancer pulmonary metastasis. |
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. |
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 | ||
分子式 | C27H28N2O3S | 分子量 | 460.59 |
溶解度 | DMSO: 250 mg/mL (542.78 mM) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.1711 mL | 10.8556 mL | 21.7113 mL |
5 mM | 0.4342 mL | 2.1711 mL | 4.3423 mL |
10 mM | 0.2171 mL | 1.0856 mL | 2.1711 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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