| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
DHP-B effectively inhibited the proliferation of CRC cell lines SW620, LS513, HCT116, RKO and LS180, with IC50 values ranging from 1.8 to 6.8 μM, and showed low toxicity to normal human colonic epithelial cells NCM460, with an IC50 value of 97.1 μM[1]. DHP-B at concentrations ≥4 μM (4-12 μM; lasting 12 days) inhibited the growth of 3D spheroids in SW620 and LS513 CRC cells for 12 days; DHP-B at concentrations 5 μM (lasting 6 days) reduced the proliferation of spheroids in SW620 and LS180 cells, as evidenced by a decrease in the percentage of Ki-67 positive cells after 6 days of treatment[1]. DHP-B has a high affinity for wild-type CPT1A, with Kd = 1.62 μM, and Cys96 residues are crucial for this binding interaction[1].
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|---|---|
| ln Vivo |
DHP-B (25 mg/kg; intraperitoneal injection; once every other day for 14 days) can significantly inhibit the growth of in situ colorectal tumors, reduce tumor cell proliferation, increase tumor cell apoptosis, inhibit fatty acid oxidation in vivo, and prolong the median survival of tumor-bearing NSG mice to more than 60 days [1].
|
| Cell Assay |
Apoptosis Analysis [1]
Cell Types: SW620, LS513, HCT116, RKO, LS180 Tested Concentrations: 5 μM (multi-cell line test); 5-10 μM (SW620 dose-response test) Incubation Duration: 24 hours Experimental Results: After incubation at 5 μM for 24 hours, all tested CRC cell lines showed apoptosis, with the apoptosis rate of SW620 cells exceeding 50%. In SW620 cells, the compound induced apoptosis in a dose-dependent manner, and the apoptosis rates at 5 μM and 10 μM concentrations were significantly higher than those at the control group. |
| Animal Protocol |
Animal/Disease Models:NOD-PrkdcscidIl2rgem1/Smoc (NSG) (8-12 weeks old) [1]
Doses: 25 mg/kg Route of Administration: Intraperitoneal injection; every other day for 14 days Experimental Results: Compared with the vector control group, rectal tumor weight was significantly reduced. The percentage of Ki-67 positive (proliferative) cells in tumor tissue was significantly reduced. The median survival of mice was extended to more than 60 days (36 days in the vector control group). Enhanced Oil Red O staining in tumor sections indicated that fatty acid oxidation was inhibited, leading to fatty acid accumulation. |
| References |
| Molecular Formula |
C23H24O8
|
|---|---|
| Molecular Weight |
428.43
|
| CAS # |
1186292-00-1
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
COC1=C(OCO2)C2=CC([C@@H]([C@@]3([H])C(C(OC3)=O)=C)C4=CC(OC)=C(C(OC)=C4)OC)=C1
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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 | 2.3341 mL | 11.6705 mL | 23.3410 mL | |
| 5 mM | 0.4668 mL | 2.3341 mL | 4.6682 mL | |
| 10 mM | 0.2334 mL | 1.1671 mL | 2.3341 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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