| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
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| ln Vitro |
Lappaol F (72 hours) causes cell fluorescence and inhibits the growth of HeLa, MDA-MB-231, SW480, and PC3 cells with IC50 values of 41.5, 26.0, 45.3, and 42.9 μM, respectively[1]. Reduces the expression levels of YAP and its target genes in HeLa, MDA-MB-231, SW480, and PC3 cells [12/24/36 h]; in addition, Lappaol F (0-50 μM, 24-72 hours) decreases the amounts of YAP protein, nuclear localization, and regulatory activity in HeLa cells [1]. Using 50 μM during 24-72 hours, Lappaol F induces MDA- and HeLa. G1 and G2 cell cycle marketing is seen in MB-231 and MCF-7 cells [2]. fluorescent imaging [1]
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|---|---|
| ln Vivo |
Human liver cancer (SW480) xenograft tumors in nude mice are inhibited in their growth by lappazol F (10 and 20 mg/kg/d) administered intravenously for 15 days [1].
|
| Cell Assay |
Immunofluorescence [1]
Cell Types: HeLa cells Tested Concentrations: 50 μM Incubation Duration: 48 h Experimental Results: The nuclear accumulation of YAP was diminished. Western Blot Analysis [2] Cell Types: HeLa, MDA-MB-231, MCF-7 Cell Tested Concentrations: 50 μM Incubation Duration: 24, 48, 72 h Experimental Results: p21 and p27 levels increased, CDK2, cyclin levels diminished B1 and CDK1. RT-PCR[1] Cell Types: HeLa, MDA-MB-231, SW480 and PC3 Cell Tested Concentrations: 50 μM Incubation Duration: 12/24/36 h Experimental Results: YAP and its target genes (such as BIRC5, BIRC5, GLI2, c -Myc, Bcl-2, Axin2 and AREG). 14-3-3σ mRNA levels were upregulated. |
| Animal Protocol |
Animal/Disease Models: Human colon cancer (SW480) nude mouse xenograft mouse [1]
Doses: 10 and 20 mg/kg/d Route of Administration: intravenous (iv) (iv)injection, 15 days Experimental Results: 48% inhibition of tumor size (10 mg/kg/ d) and 55% (20 mg/kg/d) without affecting body weight. Induces apoptosis in tumor tissue. Upregulates the level of 14-3-3σ in tumor tissue and downregulates the level of YAP. |
| References | |
| Additional Infomation |
Lappaol F has been reported in Arctium lappa with data available.
See also: Arctium lappa fruit (part of). |
| Molecular Formula |
C40H42O12
|
|---|---|
| Molecular Weight |
714.75428
|
| Exact Mass |
714.267
|
| CAS # |
69394-17-8
|
| PubChem CID |
73425459
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.5
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
52
|
| Complexity |
1170
|
| Defined Atom Stereocenter Count |
6
|
| SMILES |
O=C1OC[C@H](CC2=CC(OC)=C(O[C@H](C3=CC=C(O)C(OC)=C3)[C@H]4CO)C4=C2)[C@H]1CC5=CC(OC)=C(O[C@H](C6=CC=C(O)C(OC)=C6)[C@H]7CO)C7=C5
|
| InChi Key |
YXNKOCZXAVTXTG-NYGVLQSXSA-N
|
| InChi Code |
InChI=1S/C40H42O12/c1-46-32-15-22(5-7-30(32)43)36-28(17-41)26-11-20(13-34(48-3)38(26)51-36)9-24-19-50-40(45)25(24)10-21-12-27-29(18-42)37(52-39(27)35(14-21)49-4)23-6-8-31(44)33(16-23)47-2/h5-8,11-16,24-25,28-29,36-37,41-44H,9-10,17-19H2,1-4H3/t24-,25+,28-,29-,36+,37+/m0/s1
|
| Chemical Name |
(3R,4R)-3,4-bis[[(2S,3R)-2-(4-hydroxy-3-methoxyphenyl)-3-(hydroxymethyl)-7-methoxy-2,3-dihydro-1-benzofuran-5-yl]methyl]oxolan-2-one
|
| 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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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
|
|---|---|
| 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 | 1.3991 mL | 6.9955 mL | 13.9909 mL | |
| 5 mM | 0.2798 mL | 1.3991 mL | 2.7982 mL | |
| 10 mM | 0.1399 mL | 0.6995 mL | 1.3991 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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