W4275
Based on 1 Customer Validation
W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research.
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- Pureté: 98.93%
- CAS No.: 3051650-00-8
- Formule: C25H36N6O3
- Masse moléculaire:468.59
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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NSD2 17 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KMS-11 | IC50 |
17 μM
Compound: 42
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Antiproliferative activity against human KMS-11 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
Antiproliferative activity against human KMS-11 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
|
[PMID: 39230932] |
| MOLM-13 | IC50 |
1.199 μM
Compound: 42
|
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
|
[PMID: 39230932] |
| MOLT-4 | IC50 |
1.752 μM
Compound: 42
|
Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
|
[PMID: 39230932] |
| MV4-11 | IC50 |
1.384 μM
Compound: 42
|
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
|
[PMID: 39230932] |
| RS4-11 | IC50 |
0.23 μM
Compound: 42
|
Antiproliferative activity against human RS4-11 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
Antiproliferative activity against human RS4-11 cells assessed as inhibition of cell proliferation incubated for 6 days by CCK-8 assay
|
[PMID: 39230932] |
Chemical Information
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CAS No. 3051650-00-8
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Appearance Solid
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Masse moléculaire 468.59
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Formule C25H36N6O3
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Color White to off-white
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SMILES
CC(N1CCC(NC2=NC(C#N)=NC3=CC(OCCCN4CCOCC4)=C(C=C32)OC)CC1)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 125 mg/mL (266.76 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. 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. 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: ≥ 6.25 mg/mL (13.34 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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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-
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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.
Pureté et documentation
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Fiche technique (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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. 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 | 2.1341 mL | 10.6703 mL | 21.3406 mL | 53.3515 mL |
| 5 mM | 0.4268 mL | 2.1341 mL | 4.2681 mL | 10.6703 mL | |
| 10 mM | 0.2134 mL | 1.0670 mL | 2.1341 mL | 5.3352 mL | |
| 15 mM | 0.1423 mL | 0.7114 mL | 1.4227 mL | 3.5568 mL | |
| 20 mM | 0.1067 mL | 0.5335 mL | 1.0670 mL | 2.6676 mL | |
| 25 mM | 0.0854 mL | 0.4268 mL | 0.8536 mL | 2.1341 mL | |
| 30 mM | 0.0711 mL | 0.3557 mL | 0.7114 mL | 1.7784 mL | |
| 40 mM | 0.0534 mL | 0.2668 mL | 0.5335 mL | 1.3338 mL | |
| 50 mM | 0.0427 mL | 0.2134 mL | 0.4268 mL | 1.0670 mL | |
| 60 mM | 0.0356 mL | 0.1778 mL | 0.3557 mL | 0.8892 mL | |
| 80 mM | 0.0267 mL | 0.1334 mL | 0.2668 mL | 0.6669 mL | |
| 100 mM | 0.0213 mL | 0.1067 mL | 0.2134 mL | 0.5335 mL |