| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
|
Mensacarcin is a novel and highly potent complex polyketide acting as an an antibiotic with anticancer activity. It can be used as a cytotoxic warhead for antibody-drug conjugates (ADCs). Mensacarcin is a highly oxygenated polyketide that was first isolated from soil-dwelling Streptomyces bacteria. It exhibits potent cytostatic properties (mean of 50% growth inhibition = 0.2 μm) in almost all cell lines of the National Cancer Institute (NCI)-60 cell line screen and relatively selective cytotoxicity against melanoma cells. It strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanoma cells. Mensacarcin targets to mitochondria, affects energy metabolism in mitochondria, and activates caspase-dependent apoptotic pathways.
| ln Vitro |
On melanoma cells, mensacarcin (0-100 μM; 24 hours) exerts some cytotoxic effects but also general cytostatic effects [1]. Melanoma cells undergo fast apoptotic cell death when exposed to mensacarcin (2-50 μM) for 15 hours [1]. Mensacarcin is relatively selective for melanoma cells of cytotoxicity and demonstrates strong cytostatic capabilities (50% growth inhibition mean = 0.2 μM) in almost all cell lines examined by the National Cancer Institute (NCI)-60 cell line. A high-oxygen polyketide called mensacarcin was initially identified in soil Streptomyces sp. In melanoma cells, mensacarcin reduces mitochondrial function [1].
|
|---|---|
| Cell Assay |
Cell viability assay[1]
Cell Types: SK-Mel-28 and SK-Mel-5 melanoma cells, HCT-116 colon cancer cells Tested Concentrations: 0.01, 0.1, 1, 10, 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induction Concentration-time-dependent cell death in two melanoma cell lines tested. HCT-116 colon cancer cells were strongly inhibited. Western Blot Analysis[1] Cell Types: SK-Mel-28, SK-Mel-5 Cell Tested Concentrations: 2, 10, 50 μM Incubation Duration: 15 hrs (hours) Experimental Results: Induced formation of 89-kDa PARP-1 fragment and SK-Mel- 28 and caspase-3 in SK-Mel-5 become activated between 6 and 15 h after exposure. |
| References |
|
| Additional Infomation |
Mensacarcin has been reported in Streptomyces bottropensis with data available.
|
| Molecular Formula |
C21H24O9
|
|---|---|
| Molecular Weight |
420.41
|
| Exact Mass |
420.142
|
| CAS # |
808750-39-2
|
| PubChem CID |
403671
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
656.8±55.0 °C at 760 mmHg
|
| Flash Point |
232.9±25.0 °C
|
| Vapour Pressure |
0.0±2.1 mmHg at 25°C
|
| Index of Refraction |
1.647
|
| LogP |
5.48
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
30
|
| Complexity |
786
|
| Defined Atom Stereocenter Count |
9
|
| SMILES |
COC1c2c(OC)cccc2C(=O)C23OC12C(O)C(O)(C(C)C3O)C(=O)C1OC1C
|
| InChi Key |
WWNXYRCJJRRWAQ-ALCXHWRFSA-N
|
| InChi Code |
InChI=1S/C21H24O9/c1-8-14(22)20-15(23)10-6-5-7-11(27-3)12(10)17(28-4)21(20,30-20)18(25)19(8,26)16(24)13-9(2)29-13/h5-9,13-14,17-18,22,25-26H,1-4H3/t8-,9-,13+,14+,17-,18-,19+,20+,21+/m0/s1
|
| Chemical Name |
(1S,9S,10S,11S,12S,13S,14R)-11,12,14-trihydroxy-7,9-dimethoxy-13-methyl-12-[(2R,3S)-3-methyloxirane-2-carbonyl]-15-oxatetracyclo[8.4.1.01,10.03,8]pentadeca-3(8),4,6-trien-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 |
| 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 | 2.3786 mL | 11.8932 mL | 23.7863 mL | |
| 5 mM | 0.4757 mL | 2.3786 mL | 4.7573 mL | |
| 10 mM | 0.2379 mL | 1.1893 mL | 2.3786 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
