| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
DDO-4033 showed antiproliferative activity against 786-O, A498, A549 and HK-2 cells, with IC50 values of 1.1, 0.68, 19.96 and 18.78 μM, respectively, but its antiproliferative activity against HepG2 cells was weak, with IC50 > 50 μM [1]. DDO-4033 (0-3 μM, 0-32 h) could inhibit SPOP-mediated LATS1 ubiquitination and degradation, and downregulate the mRNA levels of CTGF and CYR61 genes in A498 cells [1]. DDO-4033 (0-5 μM, 24 h) could inhibit colony formation of A498 cells and impair their migration ability [1]. DDO-4033 showed affinity for SPOP under MST, BLI and ITC detection, with Kd values of 15.1, 4.96 and 4.94 μM, respectively [1].
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| ln Vivo |
DDO-4033 (10-50 mg/kg, intratumoral (it) and peritumoral (PTI), once daily for 3 weeks) inhibited tumor growth, upregulated LATS1, and activated the Hippo pathway in the A498-Luc xenograft BALB/c nude mouse model [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: A498 cells Tested Concentrations: 0 μM, 0.12 μM, 0.25 μM, 0.5 μM, 1 μM Incubation Duration: 0 h, 1 h, 2 h, 4 h, 8 h, 12 h, 16 h, 32 h Experimental Results: Inhibited LATS1 ubiquitination, prolonged the half-life of LATS1, and led to LATS1 accumulation. Cell migration assay [1] Cell Types: A498 cells Tested Concentrations: 0 μM, 0.5 μM, 1 μM Incubation Duration: 24 hours Experimental Results: Inhibited colony formation and impaired cell migration ability. |
| Animal Protocol |
Animal/Disease Models:A498-Luc (1 × 10⁷ cells, containing 25% Matrigel, subcutaneous injection) xenograft BALB/c nude mouse (female, 18-20 g, 4-6 weeks old) model [1]
Doses: 10 mg/kg, 50 mg/kg Route of Administration: Once daily for 3 weeks Experimental Results: Inhibited tumor growth, upregulated LATS1 and activated the Hippo pathway, with low toxicity and no alteration of organ tissues. |
| References |
| Molecular Formula |
C20H18N6O4
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|---|---|
| Molecular Weight |
406.39
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| Appearance |
White to off-white solid
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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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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~61.52 mM; ultrasonic and warming and heat to 60°C)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Suspended solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4607 mL | 12.3035 mL | 24.6069 mL | |
| 5 mM | 0.4921 mL | 2.4607 mL | 4.9214 mL | |
| 10 mM | 0.2461 mL | 1.2303 mL | 2.4607 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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