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250mg | ||
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Other Sizes |
ln Vitro |
In roughly 72 hours, CHNQD-01255 (0-1 μM) suppresses the growth of HepG2 and BEL-7402 cells[1].
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ln Vivo |
HepG2 tumor-bearing xenograft mice showing tumor growth inhibition are treated with CHNQD-01255 (5–45 mg/kg, po)[1]. With MTD values for po and ip doses in mice above 750 and 100 mg/kg, CHNQD-01255 demonstrates a strong safety profile[1].
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Cell Assay |
Cell Proliferation AssayCHNQD-01255 (0-1 μM approximately, 72 h) inhibits HepG2 and BEL-7402 cell proliferation[1].
Cell Types: HepG2, BEL-7402 cell Tested Concentrations: 0-1 μM approximately Incubation Duration: 72 h Experimental Results: Inhibited cell proliferation with an IC50 value of 0.1 μM (HepG2) and 0.07 μM (BEL-7402). |
Animal Protocol |
Animal/Disease Models: HepG2 tumor-bearing xenograft mice[1]
Doses: 5, 15, and 45 mg/kg Route of Administration: Oral adminstration (po), every day for 21 days. Experimental Results: Resulted in dramatically delayed tumor progression, with a tumor growth inhibition rate (TGI %) value of 61.0% at 45 mg/kg. Animal/Disease Models: HepG2 tumor-bearing xenograft mice[1] Doses: 1 and 9 mg/kg Route of Administration: intraperitoneal (ip) injection , every day for 21 days. Experimental Results: Inhibited the tumor growth with the TGI values of 36.6 and 48.3%, respectively. Animal/Disease Models: Mice (pharmacokinetic/PK assay)[1] Doses: 45 mg/kg po, 10 mg/kg iv Route of Administration: Oral adminstration (po) or intravenous (iv) injection Experimental Results: pharmacokinetic/PK profile of CHNQD-01255. dose (mg/kg) T1/2 (h) Cmax (ng/mL) Cl (mL/h/kg) F ( %) 45 (po) 7.35 20.26 598245.37 2.26 10 (iv) 2060.78 |
References |
[1]. Yao-Yao Jiang, et al. Design and Characterization of a Natural Arf-GEFs Inhibitor Prodrug CHNQD-01255 with Potent Anti-Hepatocellular Carcinoma Efficacy In Vivo. J Med Chem. 2022 Sep 22;65(18):11970-11984.
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Molecular Formula |
C23H29NO6
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Molecular Weight |
415.48
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CAS # |
2756173-91-6
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Appearance |
Typically exists as solids (or liquids in special cases) 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 | 2.4069 mL | 12.0343 mL | 24.0685 mL | |
5 mM | 0.4814 mL | 2.4069 mL | 4.8137 mL | |
10 mM | 0.2407 mL | 1.2034 mL | 2.4069 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.