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250mg | ||
500mg | ||
Other Sizes |
ln Vitro |
FK-3000 (0-5 μg/mL; 48 h) restricts the growth of cells; the IC50 values for MCF-7, PC-3, A-431, HT-29, and CT-26 cells are, in turn, 0.52 μg/mL, 0.77 μg/mL, 0.22 μg/mL, 2.70 μg/mL, and 1.90 μg/mL[1]. MDA-MB-231 cells undergo apoptosis when exposed to FK-3000 (0.5-5.0 μg/mL; 24-48 h) in a dose- and time-dependent manner[1]. In MDA-MB-231 and MCF-7 cells, FK-3000 (0.5-5.0 μg/mL; 24-48 h) promotes G2/M phase arrest in a dose- and time-dependent manner [2]. In MDA-MB-231 cells, FK-3000 (0.5-5.0 μg/mL; 60-120 min or 24-48 h) decreases COX-2 expression and NF-κB phosphorylation levels [1]. In MDA-MB-231 cells, FK-3000 (5.0 μg/mL; 120 min) efficiently inhibits NF-κB's translocation from the cytoplasm to the nucleus [1].
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ln Vivo |
In an MDA-MB-231 xenograft mice model, FK-3000 (1 mg/kg/day; ip daily for 24 d) suppresses tumor growth without exhibiting any harm [1]. FK-3000 (10–25 mg/kg; po for 10 d) considerably postpones skin damage, prevents more damage from developing, and increases the average survival duration of HSV-1-infected mice [3].
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References |
[1]. Xu HD, et, al. FK-3000 isolated from Stephania delavayi Diels. inhibits MDA-MB-231 cell proliferation by decreasing NF-κB phosphorylation and COX-2 expression. Int J Oncol. 2015;46(6):2309-16.
[2]. Li YC, et, al. 6,7-di-O-acetylsinococuline (FK-3000) induces G2/M phase arrest in breast carcinomas through p38 MAPK phosphorylation and CDC25B dephosphorylation. Int J Oncol. 2015 Feb;46(2):578-86. [3]. Nawawi A, et, al. In vivo antiviral activity of Stephania cepharantha against herpes simplex virus type-1. Phytother Res. 2001 Sep;15(6):497-500. [4]. Lee JH, et, al. Development of a LC-MS method for quantification of FK-3000 and its application to in vivo pharmacokinetic study in drug development. J Pharm Biomed Anal. 2012 Nov;70:587-91. |
Molecular Formula |
C22H27NO7
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Molecular Weight |
417.45
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CAS # |
1054312-81-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(C)O[C@@H]1C(OC)=C2[C@@H]3CC4C=CC(=C(O)C=4[C@]2(CCN3)C[C@@H]1OC(C)=O)OC
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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 | 2.3955 mL | 11.9775 mL | 23.9550 mL | |
5 mM | 0.4791 mL | 2.3955 mL | 4.7910 mL | |
10 mM | 0.2395 mL | 1.1977 mL | 2.3955 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.