WJ460 |
| رقم الكتالوجGC38203 |
WJ460 هو مثبط قوي من myoferlin (MYOF) ، والذي يتفاعل مباشرة مع MYOF ويمارس نشاطًا مضادًا للنقائل في النطاق النانوي في خلايا سرطان الثدي
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.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
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.
|
Cell experiment[1]: |
|
|
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]: |
|
|
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 | ||
| Formula | C27H28N2O3S | M.Wt | 460.59 |
| الذوبان | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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 ddH2O, 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *