W23-1006
Based on 1 Customer Validation
W23-1006 is a selective and covalent ALKBH5 inhibitor. W23-1006 binds to the ALKBH5 C200 residue with an IC50 value of 3.848 μM. W23-1006 shows ~30- and 8-fold stronger inhibitory activity than that against FTO and ALKBH3, respectively. W23-1006 can be used for the study of triple-negative breast cancer (TNBC).
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- Purity: 97.15%
- CAS No.: 3035498-92-8
- 화학식: C17H12BrN3O5
- 분자량:418.20
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보관:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
W23-1006 (5 μM; 24 h) significantly increases the mA abundance in MDA-MB-231 and BT549 cells[1].
W23-1006 (3.16-31.6 μM; 24 h) inhibits the cell viability of MDA-MB-231 and BT549[1].
W23-1006 (5 μM) could obviously reduce TNBC cell colonization area and suppress cell migration[1].
W23-1006 (5-10 μM) induces the apoptosis and decreases the G2/M phase of MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 and BT549 cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:The mA abundance significantly increased in cells.
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Cell Line:MDA-MB-231 and BT549 cells
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Concentration:3.16 μM, 10 μM, 31.62 μM
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Incubation Time:24 h
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Result:Inhibited cell viability of MDA-MB-231 and BT549 with IC50 values of 10.31 μM and 6.338 μM, respectively.
W23-1006 (25 mg/kg; i.p.; once daily; for 10 days) could obviously inhibit TNBC lung metastasis[1].
W23-1006 (single dosage at 25 mg/kg; i.p.) shows the t1/2 ranged from 0.509 to 0.983 h, and the Cmax in plasma (in the range of 1715-2108 ng/mL) is reached 15 min in mice[1].
Neither 100 mg/kg nor 250 mg/kg dosage of W23-1006 (i.p.) causes adverse events or death in KM mice (22-27g)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Immunodefcient female mouse was subcutaneously injected MDA-MB-231 cells[1].
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Dosage:25 mg/kg (5% DMSO, 10% Kolliphor HS 15, and 85% saline)
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Administration:Intraperitoneal injection; once daily; for 14 days
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Result:Apparently reduced the tumor volume and weight.
Strongly reduced the FN1 and Ki-67 protein expression level.
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Animal Model:Immunodefcient female mouse injected MDA-MB-231LMF3 through the tail vein[1].
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Dosage:25 mg/kg
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Administration:Intraperitoneal injection; once daily; for 10 days
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Result:Inhibited TNBC lung metastasis.
No apparent pathologic abnormality was observed in the HEstaining results of multiple organs, including heart, liver,spleen, lung, and kidney.
There was no signifcant diference in glutamic pyruvic transaminase(ALT) and glutamic oxaloacetic transaminase (AST) levels in mouse serum, did not infuence mice liver function.
Chemical Information
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CAS No. 3035498-92-8
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Appearance Solid
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분자량 418.20
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화학식 C17H12BrN3O5
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Color Brown to reddish brown
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SMILES
O=C(/C1=C\C2=CC([N+]([O-])=O)=CC(Br)=C2)NN(C3=CC=C(C=C3)OC)C1=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
용액&용해도
DMSO : 100 mg/mL (239.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (stored under nitrogen). 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 (stored under nitrogen). 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 (5.98 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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 (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 (stored under nitrogen). 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 | 2.3912 mL | 11.9560 mL | 23.9120 mL | 59.7800 mL |
| 5 mM | 0.4782 mL | 2.3912 mL | 4.7824 mL | 11.9560 mL | |
| 10 mM | 0.2391 mL | 1.1956 mL | 2.3912 mL | 5.9780 mL | |
| 15 mM | 0.1594 mL | 0.7971 mL | 1.5941 mL | 3.9853 mL | |
| 20 mM | 0.1196 mL | 0.5978 mL | 1.1956 mL | 2.9890 mL | |
| 25 mM | 0.0956 mL | 0.4782 mL | 0.9565 mL | 2.3912 mL | |
| 30 mM | 0.0797 mL | 0.3985 mL | 0.7971 mL | 1.9927 mL | |
| 40 mM | 0.0598 mL | 0.2989 mL | 0.5978 mL | 1.4945 mL | |
| 50 mM | 0.0478 mL | 0.2391 mL | 0.4782 mL | 1.1956 mL | |
| 60 mM | 0.0399 mL | 0.1993 mL | 0.3985 mL | 0.9963 mL | |
| 80 mM | 0.0299 mL | 0.1495 mL | 0.2989 mL | 0.7473 mL | |
| 100 mM | 0.0239 mL | 0.1196 mL | 0.2391 mL | 0.5978 mL |
W23-1006 Related Classifications
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