| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
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| ln Vitro |
Rubone (0-60 μM) exhibits significant cytotoxicity in DU145-TXR and PC3-TXR cells, suggesting a strong anticancer effect of Rubone in late-stage TRUC cells, which have lower miR-34a Rubone (5, 10 uM; 48 hours) significantly reversed the expression of miR-34a downstream gene targets in DU145-TXR and PC3-TXR cell lines. Rubone upregulates PTX-resistant DU145-TXR expression in a dose-model manner [3]. Rubone (5 μM; for 2 weeks) and PTX (for 2 weeks) combined inhibit PC3-TXR cell growth and spheroid formation in 3D models, including miR-34a in apical 3D and PC3-TXR cell lines [3]. Combination treatment with Rubone and PTX inhibits p53 to achieve independence in cell proximity, migration, and cancer stem-like cell (CSC) populations. Rubone monotherapy or combination of Rubone and PTX significantly enhanced the expression of TAp73 and Elk-1[3]
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|---|---|
| ln Vivo |
In addition to inhibiting tumor growth, rubone monotherapy (PEG-PCD micelles loaded with drug 20 mg/kg; daily intravenous injection; five doses total) or coupled with PTX (PEG-PCD micelles loaded with drug 10 mg/kg) dramatically increased tumors. The growth of tumor cells is inhibited by rubone alone [3].
|
| Cell Assay |
cytotoxicity assay[3]
Cell Types: DU145, PC3, PTX-resistant DU145-TXR, PC3-TXR, LNCaP, C4 developed by LNCaP -2 Cell Tested Concentrations: 0-60 μM Incubation Duration: Experimental Results: demonstrated Dramatically higher cytotoxicity in . DU145-TXR and PC3-TXR cells. Western Blot Analysis[3] Cell Types: DU145-TXR and PC3-TXR Cell lines Tested Concentrations: 5, 10 uM Incubation Duration: 48 hrs (hours) Experimental Results: Dramatically reversed the expression of miR-34a downstream target genes of DU145-TXR and PC3-TXR cell lines, including E-cadherin, SIRT1 and Cyclin D1, while E-cadherin expression was not reversed in the DU145-TXR cell line. Real-time qPCR[3] Cell Types: DU145-TXR and PC3-TXR cell lines Tested Concentrations: 5, 10 uM Incubation Duration: 48 hrs (hours) Experimental Results: Dose-dependent upregulation of miR-34a in PTX-resistant DU145-TXR and PC3-TXR cell lines Way. |
| Animal Protocol |
Animal/Disease Models: 8weeks old male nude mice transfected with prostate cancer cells [3]
Doses: 20 mg/kg or 10 mg/kg Each drug (PTX and Rubone) loaded with PEG-PCD Micellar Route of Administration: intravenous (iv) (iv)injection, every Results of 5 doses given every other day: had little effect on weight loss and inhibited tumor growth. Monotherapy or combined treatment with PTX Dramatically upregulated the expression of miR-34a in tumors. The expression of E-cadherin, cyclin D1, and SIRT1 was Dramatically reversed by PTX alone or in combination with PTX. |
| References | |
| Additional Infomation |
Rubone is a member of chalcones.
|
| Molecular Formula |
C20H22O7
|
|---|---|
| Molecular Weight |
374.38448
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| Exact Mass |
374.137
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| CAS # |
73694-15-2
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| Related CAS # |
73694-15-2;
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| PubChem CID |
5951499
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| Appearance |
Light yellow to yellow solid powder
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| Index of Refraction |
1.578
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| LogP |
3.331
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
27
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| Complexity |
495
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=CC(=C(C(=C1)OC)C(=O)/C=C/C2=CC(=C(C=C2OC)OC)OC)O
|
| InChi Key |
VHCQVGQULWFQTM-VOTSOKGWSA-N
|
| InChi Code |
InChI=1S/C20H22O7/c1-23-13-9-15(22)20(19(10-13)27-5)14(21)7-6-12-8-17(25-3)18(26-4)11-16(12)24-2/h6-11,22H,1-5H3/b7-6+
|
| Chemical Name |
(E)-1-(2-hydroxy-4,6-dimethoxyphenyl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6711 mL | 13.3554 mL | 26.7108 mL | |
| 5 mM | 0.5342 mL | 2.6711 mL | 5.3422 mL | |
| 10 mM | 0.2671 mL | 1.3355 mL | 2.6711 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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