YL-5092
Based on 1 Customer Validation
YL-5092 is a selective YT521-B homology (YTH) domain-containing protein 1 (YTHDC1) inhibitor with an IC50 of 7.4 nM and a KD of 29.6 nM. YL-5092 can suppress cancer cell proliferation and induce cell G0/G1 phase arrest and apoptosis. YL-5092 can be used for the research of cancer, such as acute myeloid leukemia (AML).
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- Pureté: 99.83%
- CAS No.: 3056857-07-6
- Formule: C22H14F3N3O2S
- Masse moléculaire:441.43
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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YTHDC1 7.4 nM (IC50) |
YTHDC1 29.6 nM (Kd) |
YL-5092 inhibits acute myeloid leukemia cell with IC50 values of 0.28-2.87 μM[1].
YL-5092 (0.1-30 μM, 6 h) stabilizes YTHDC1 in MOLM-13 and U937 cells[1].
YL-5092 (1 μM) blocks the binding of YTHDC1 with its substrates (m6A-mRNAs) in HEK293T cells[1].
YL-5092 (1 μM) reduces MYC mRNA levels in MOLM-13 cells[1].
YL-5092 (0.25-2 μM, 48-120 h) induces G0/G1 phase arrest and increases apoptotic cells in MOLM-13 cells[1].
YL-5092 (1-3 μM, 14-16 days) inhibits the colony-forming ability of CD34+ cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM-13 cells
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Concentration:0.25, 0.5, 1 and 2 μM
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Incubation Time:48 h
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Result:Increased cells in G0/G1 phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse MOLM-13/U937 tumor xenograft models[1]
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Dosage:70 mg/kg
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Administration:Intraperitoneally injection, twice a day for 18 days
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Result:Alleviated the development of leukemia and significantly prolonged the survival rate of mice.
Reduced leukemia infiltration in the peripheral blood, spleen, and bone marrow.
Reduced the expression of YTHDC1 target genes, including MYC, FOXM1, GINS1, MCM2, MCM4 and MCM5.
Had no weight loss.
Chemical Information
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CAS No. 3056857-07-6
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Appearance Solid
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Masse moléculaire 441.43
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Formule C22H14F3N3O2S
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Color Light yellow to yellow
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SMILES
O=C(C1=CNC(C(NC2=CC=C(C3=CN=CS3)C=C2)=O)=C1)C4=C(C(F)(F)F)C=CC=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (226.54 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: ≥ 2.5 mg/mL (5.66 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.
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 (273 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 | 2.2654 mL | 11.3268 mL | 22.6536 mL | 56.6341 mL |
| 5 mM | 0.4531 mL | 2.2654 mL | 4.5307 mL | 11.3268 mL | |
| 10 mM | 0.2265 mL | 1.1327 mL | 2.2654 mL | 5.6634 mL | |
| 15 mM | 0.1510 mL | 0.7551 mL | 1.5102 mL | 3.7756 mL | |
| 20 mM | 0.1133 mL | 0.5663 mL | 1.1327 mL | 2.8317 mL | |
| 25 mM | 0.0906 mL | 0.4531 mL | 0.9061 mL | 2.2654 mL | |
| 30 mM | 0.0755 mL | 0.3776 mL | 0.7551 mL | 1.8878 mL | |
| 40 mM | 0.0566 mL | 0.2832 mL | 0.5663 mL | 1.4159 mL | |
| 50 mM | 0.0453 mL | 0.2265 mL | 0.4531 mL | 1.1327 mL | |
| 60 mM | 0.0378 mL | 0.1888 mL | 0.3776 mL | 0.9439 mL | |
| 80 mM | 0.0283 mL | 0.1416 mL | 0.2832 mL | 0.7079 mL | |
| 100 mM | 0.0227 mL | 0.1133 mL | 0.2265 mL | 0.5663 mL |
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