| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
CHNQD-03301 (Compound 20) (0.01-1.0 μM, 24 hours) dose-dependently reduced HIF-1α protein levels in HCT116 cells and decreased the expression of downstream target proteins CA9, REDD1, and PDK1. Simultaneously, the mRNA expression levels of downstream genes such as CA9, VEGF, and REDD1 were also significantly reduced [1]. CHNQD-03301 (0.4-1.6 μM) significantly reduced EPO mRNA levels and inhibited hypoxia-induced angiogenesis in HCT116 cells [1]. The IC50 value of CHNQD-03301 in HCT116 cells was 2.31 μM under normoxic conditions and 0.83 μM under hypoxic conditions [1]. CHNQD-03301 (0.4-1.6 μM) induced cell cycle arrest in HCT116 cells at the G2 phase under hypoxic conditions [1]. CHNQD-03301 (0.4-1.6 μM) had no significant effect on the proliferation of HCT116 cells, but significantly inhibited the proliferation of von Hippel-Lindau (VHL) deficient RCC4 cells [1]. CHNQD-03301 (1-4 μM, 7-14 days) inhibited the formation of spheroids in HCT116 cells in a dose-dependent manner [1]. CHNQD-03301 (0.4-2.0 μM, 24 hours) significantly inhibited the migration ability of HCT116 cells and VHL deficient RCC4 cells under hypoxic conditions [1].
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| ln Vivo |
CHNQD-03301 (Compound 20) (1 mg/kg, face, once daily, 13-19 days) significantly inhibited the growth of MB49 allogeneic xenografts and HCT116 xenografts in mice without significant toxicity [1]. CHNQD-03301 (100 mg/kg, face, single dose) did not show acute toxicity in mice at a dose of 100 mg/kg, and the maximum tolerated dose (MTD) was 100 mg/kg, indicating that it has good safety [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HCT116 cells, RCC4 cells Tested Concentrations: 0.01 μM, 0.1 μM, 1.0 μM Incubation Duration: 24 h Experimental Results: In HCT116 cells, CHNQD-03301 dose-dependently reduced HIF-1α protein levels and decreased the expression of downstream target proteins (CA9, REDD1, PDK1). In HCT116 cells exogenously overexpressing HIF-1α, CHNQD-03301 also reduced HIF-1α protein levels. In RCC4 cells (VHL-deficient), CHNQD-03301 effectively reduced HIF-1α and CA9 protein levels. Co-treatment with the proteasome inhibitor MG132 rescued CHNQD-03301-induced HIF-1α degradation. Cell Migration Assay [1] Cell Types: HCT116 cells (under hypoxic conditions), VHL-deficient RCC4 cells Tested Concentrations: 0.4 μM, 0.8 μM, 1.6 μM Incubation Duration: 24 h Experimental Results: Significantly inhibited the migration ability of HCT116 cells under hypoxic conditions and VHL-deficient RCC4 cells. |
| Animal Protocol |
Animal/Disease Models: A tumor model was established in female C57BL/6J (8-week-old) mice by subcutaneous injection of MB49 mouse bladder cancer cells (1×105 cells/mouse)[1].
Doses: 1 mg/kg Route of Administration: P.o., once daily for 13 days Experimental Results: Low-dose oral administration effectively inhibited MB49 tumor growth (TGI = 52.0%) and showed no significant change in mouse body weight. Animal/Disease Models: A tumor model was also established in female C57BL/6J (8-week-old) mice by subcutaneous injection of HCT116 human colon cancer cells (2×106 cells/mouse)[1]. Doses: 1 mg/kg Route of Administration: P.o., once daily for 19 days Experimental Results: Low-dose oral administration effectively inhibited MB49 tumor growth (TGI = 51.0%) and showed no significant change in mouse body weight. Animal/Disease Models: Healthy female ICR mice[1]. Doses: 100 mg/kg Route of Administration: P.o., once Experimental Results: None of the mice died within 7 days. No apparent difference in blood biochemistry parameters, including ALT, AST, LDH, UREA, CREA, UA, and CK. Hematoxylin and eosin (H&E) staining results presented no pathological changes in the collected tissues (hearts, livers, spleens, lungs, kidneys, and duodenum). |
| References |
| Molecular Formula |
C23H20O6
|
|---|---|
| Molecular Weight |
392.40
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| CAS # |
3104302-65-7
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| Appearance |
Typically exists as solids at room temperature
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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 | 2.5484 mL | 12.7421 mL | 25.4842 mL | |
| 5 mM | 0.5097 mL | 2.5484 mL | 5.0968 mL | |
| 10 mM | 0.2548 mL | 1.2742 mL | 2.5484 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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