LLK203
Based on 1 Customer Validation
LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model.
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- Purity: 98.58%
- CAS No.: 2758090-62-7
- 화학식: C28H23N3O4S3
- 분자량:561.69
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보관:Powder -20°C, 3 years , 4°C, 2 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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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USP2 0.89 μM (IC50) |
USP8 0.52 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF-10A | IC50 |
20.4 μM
Compound: LLK203
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Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38452725] |
| MCF7 | IC50 |
3.4 μM
Compound: LLK203
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38452725] |
LLK203 (0-100 μM; 36 h) demonstrates high inhibitory activity on MCF-7 cells (IC50=3.4 μM) compared with ML364 (IC50=9.3 μM). LLK203 demonstrates a 4-fold increase in USP2 activity and a 9-fold increase in USP8 activity compared to ML364 (HY-100900)[1].
LLK203 (10-50 μM; 24 h) increases the ratio of apoptotic cells and remaines largely in G1 phas on MCF-7 cells[1].
LLK203 (2-50 μM; 24 h) can degrade various proteins (MDM2, Cyclin D1, Her2, ERα) in a dosedependent manner[1].
LLK203 (2-50 μM; for 7 days) shows a robust ability of inhibiting clone formation at the concentration of 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 and MCF10A cells
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Concentration:0-100 μM
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Incubation Time:36 h
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Result:Exhibited lower cytotoxicity towards normal cells (MCF10A; IC50=20.4 μM), while demonstrating higher inhibitory activity on BC cells (MCF-7; IC50=3.4 μM).
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Cell Line:MCF-7 cells
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Concentration:10, 30, 50 μM
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Incubation Time:24 h
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Result:Increased the ratio of apoptotic cells.
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Cell Line:MCF-7 cells
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Concentration:10, 30, 50 μM
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Incubation Time:24 h
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Result:Remained largely in G1 phase.
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Cell Line:MCF-7 cells
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Concentration:2, 5, 10, 30, 50 μM
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Incubation Time:24 h
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Result:Could degrade various proteins (MDM2, Cyclin D1, Her2, ERα) in a dosedependent manner.
Pharmacokinetic Parameters of LLK203 in male Sprague-Dawley rats[1].
| Intravenously (5 mg/kg) | Orally (50 mg/kg) | |
| Tmax (h) | 6 | |
| Cmax (ng/mL) | 36630 | 1572 |
| AUC0-t (h∗ng/mL) | 60824 | 19144 |
| T1/2 (h) | 20 | 6.14 |
| CL (mL/h/kg) | 58 | |
| F (%) | 2.2% |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice subcutaneously inoculated with 4T1 cells[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal; every day; for 23 days
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Result:Significantly reduced tumor growth in a 4T1 tumor-bearing mice model.
Chemical Information
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CAS No. 2758090-62-7
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Appearance Solid
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분자량 561.69
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화학식 C28H23N3O4S3
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Color White to off-white
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SMILES
O=C(C1=CC=C(OC)C=C1NS(=O)(C2=CC=C(C3=CC=C(C)S3)C=C2)=O)NC4=NC(C5=CC=CC=C5)=CS4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (178.03 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.
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.
순도&문서
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Data Sheet (285 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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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. 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 | 1.7803 mL | 8.9017 mL | 17.8034 mL | 44.5085 mL |
| 5 mM | 0.3561 mL | 1.7803 mL | 3.5607 mL | 8.9017 mL | |
| 10 mM | 0.1780 mL | 0.8902 mL | 1.7803 mL | 4.4509 mL | |
| 15 mM | 0.1187 mL | 0.5934 mL | 1.1869 mL | 2.9672 mL | |
| 20 mM | 0.0890 mL | 0.4451 mL | 0.8902 mL | 2.2254 mL | |
| 25 mM | 0.0712 mL | 0.3561 mL | 0.7121 mL | 1.7803 mL | |
| 30 mM | 0.0593 mL | 0.2967 mL | 0.5934 mL | 1.4836 mL | |
| 40 mM | 0.0445 mL | 0.2225 mL | 0.4451 mL | 1.1127 mL | |
| 50 mM | 0.0356 mL | 0.1780 mL | 0.3561 mL | 0.8902 mL | |
| 60 mM | 0.0297 mL | 0.1484 mL | 0.2967 mL | 0.7418 mL | |
| 80 mM | 0.0223 mL | 0.1113 mL | 0.2225 mL | 0.5564 mL | |
| 100 mM | 0.0178 mL | 0.0890 mL | 0.1780 mL | 0.4451 mL |
LLK203 Related Classifications
HY-162312 Related Classifications
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