DDO-4033
Based on 1 Customer Validation
DDO-4033 is a SPOP inhibitor (IC50 = 16.9 μM, Kd = 15.1 μM). DDO-4033 impairs the malignant migration, invasion, and proliferation of clear cell renal cell carcinoma (ccRCC) cell lines. DDO-4033 disrupts SPOP recruitment to its substrate LATS1, inhibits its polyubiquitination and subsequent degradation, and upregulates LATS1 expression. DDO-4033 has promising antitumor activity and is promising for renal cell carcinoma research.
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- Purity: 99.11%
- 화학식: C20H18N6O4
- 분자량:406.39
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Biological Activity
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Lats1 |
DDO-4033 shows antiproliferative activity against 786-O, A498, A549, HK-2 cells, with IC50s of 1.1, 0.68, 19.96, 18.78 μM, respectively, but has weak antiproliferative activity against HepG2 cells, with an IC50 > 50 μM[1].
DDO-4033 (0-3 μM, 0-32 h) inhibits SPOP-mediated LATS1 ubiquitination and degradation, downregulates the mRNA level of CTGF and CYR61 genes in A498 cells[1].
DDO-4033 (0-5 μM, 24 h) inhibits the colony formation and impairs the cell migratory capacity in A498 cells[1].
DDO-4033 shows affinity for SPOP under MST, BLI, and ITC detection, with Kds of 15.1, 4.96, 4.94 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A498 cells
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Concentration:0 μM, 0.12 μM, 0.25 μM, 0.5 μM, 1 μM
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Incubation Time:0 h, 1 h, 2 h, 4 h,8 h, 12 h, 16 h, 32 h
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Result:Inhibited LATS1 ubiquitination, prolongs the half-life of LATS1, and accumulates LATS1.
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Cell Line:A498 cells
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Concentration:0 μM, 0.5 μM, 1 μM
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Incubation Time:24 h
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Result:Inhibited the colony formation and impaired the cell migratory capacity.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A498-Luc (1 × 107 cells containing 25% Matrigel, s.c.) xenograft BALB/c nude mice (female, 18-20 g, 4-6 weeks of age) model[1]
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Dosage:10 mg/kg, 50 mg/kg
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Administration:i.t. and PTI, once daily, 3 weeks
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Result:Inhibited tumor growth, upregulated LATS1 and activated the Hippo pathway, was low in toxicity and did not change organ tissues.
Chemical Information
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Appearance Solid
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분자량 406.39
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화학식 C20H18N6O4
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Color White to off-white
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SMILES
C#CC1=C([N+]([O-])=O)C=C(C(NC2=CC(C)=NN2C(N3)=NC(CCC)=CC3=O)=O)C=C1
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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 : 25 mg/mL (61.52 mM; ultrasonic and warming and heat to 60°C; 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 (6.15 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
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.
순도&문서
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Data Sheet (280 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. 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 | 2.4607 mL | 12.3035 mL | 24.6069 mL | 61.5173 mL |
| 5 mM | 0.4921 mL | 2.4607 mL | 4.9214 mL | 12.3035 mL | |
| 10 mM | 0.2461 mL | 1.2303 mL | 2.4607 mL | 6.1517 mL | |
| 15 mM | 0.1640 mL | 0.8202 mL | 1.6405 mL | 4.1012 mL | |
| 20 mM | 0.1230 mL | 0.6152 mL | 1.2303 mL | 3.0759 mL | |
| 25 mM | 0.0984 mL | 0.4921 mL | 0.9843 mL | 2.4607 mL | |
| 30 mM | 0.0820 mL | 0.4101 mL | 0.8202 mL | 2.0506 mL | |
| 40 mM | 0.0615 mL | 0.3076 mL | 0.6152 mL | 1.5379 mL | |
| 50 mM | 0.0492 mL | 0.2461 mL | 0.4921 mL | 1.2303 mL | |
| 60 mM | 0.0410 mL | 0.2051 mL | 0.4101 mL | 1.0253 mL |
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