| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Anticancer agent 304 (compound 17) effectively inhibited the proliferation of HepG2, Huh-7 and SK-Hep-1 cells, with IC50 values of 1.5 μM, 1.1 μM and 1.1 μM, respectively [1]. Anticancer agent 304 (0.5-1.5 μM; 24 h) inhibited the colony formation and proliferation of SK-Hep-1 and Huh-7 cells, reduced the expression level of intracellular CDC45 protein, and promoted the nuclear export of CDC45 protein [1]. Anticancer agent 304 (1.56-250 μM) could directly bind to purified CDC45 protein, with a dissociation constant (Kd) of 83.0 μM [1]. Anticancer drug 304 (0.5-1.5 μM; 12 h) caused SK-Hep-1 and Huh-7 cells to arrest in the G2/M phase of the cell cycle by upregulating p27 and downregulating p-CDC2 [1]. The anticancer drug 304 (0.5-1.5 μM; 48 h) induces apoptosis in SK-Hep-1 and Huh-7 liver cancer cells by upregulating C-PARP-1 and downregulating PARP-1 and BCL-2[1]. The anticancer drug 304 (0.5-1.5 μM; 48 h) reverses epithelial-mesenchymal transition by upregulating E-cadherin and downregulating N-cadherin and vimentin, and inhibits the migration and invasion of SK-Hep-1 and Huh-7 liver cancer cells[1].
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|---|---|
| ln Vivo |
The anticancer agent 304 (30-60 mg/kg; intraperitoneal injection; daily; 51 days) showed highly effective and non-toxic anticancer activity in nude mice with xenografts of hepatocellular carcinoma, achieving tumor weight inhibition rates of 76% and 84% at doses of 30 mg/kg and 60 mg/kg, respectively, while reducing the expression of CDC45 in tumor tissue [1].
|
| Animal Protocol |
Animal/Disease Models:NU/NU nude mice (male, 4 weeks old, subcutaneously injected with Huh-7 cells)[1]
Doses: 30 mg/kg; 60 mg/kg Route of Administration: Intraperitoneal injection; once daily; for 51 days Experimental Results: The 30 mg/kg dose group showed a tumor growth inhibition rate of 73% after 51 days. The 30 mg/kg dose group showed a tumor weight reduction of 76% after 51 days. The 60 mg/kg dose group showed a tumor growth inhibition rate of 84% after 51 days. The 60 mg/kg dose group showed a tumor weight reduction of 84% after 51 days. Compared with the control group, the expression of CDC45 protein in tumor tissue was reduced. No compound-related weight changes were observed. Serum levels of liver and kidney biomarkers (ALT/GPT, AST/GOT, BUN, CRE) remained within the normal range. Histopathological analysis showed no structural abnormalities in the major organs (heart, liver, spleen, lungs, and kidneys). |
| References |
| Molecular Formula |
C42H46O8
|
|---|---|
| Molecular Weight |
678.81
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
C[C@@]1(O)C2=C([C@]3(C)C[C@H]2C[C@H]3C(C4=CC=C(C([C@H]5[C@](C[C@H]6C5)(C)C7=C6[C@@](C)(O)CC[C@@H](C8=C)[C@@H]7OC8=O)=O)C=C4)=O)[C@@H]9[C@H](C(C(O9)=O)=C)CC1
|
| 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 | 1.4732 mL | 7.3658 mL | 14.7317 mL | |
| 5 mM | 0.2946 mL | 1.4732 mL | 2.9463 mL | |
| 10 mM | 0.1473 mL | 0.7366 mL | 1.4732 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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