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| 5mg |
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| Targets |
α-Carotene is a vitamin A precursor and exhibits anticancer and antioxidant activity. It inhibits proliferation of GOTO human neuroblastoma cells more potently than β-carotene and halts the cell cycle at the G0/G1 phase.
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| ln Vitro |
In LLC cells, α-carotene (0.5-2.5 μM; 24 h) significantly and concentration-dependently enhanced the protein expression of TIMP-1 and TIMP-2. The expression of PAI-1 protein was considerably enhanced by AC (0.5-2.5 μM). Additionally, integrin β1-mediated phosphorylation of focal adhesion kinase (FAK) is greatly inhibited by α-carotene (2.5 μM), which lowers the phosphorylation of the MAPK family [2]. During 48 hours of incubation, α-Carotene (0.5, 1, 2.5 μM; 48 h) substantially and concentration-dependently reduced LLC invasion [2]. The activities of MMP-9, -2, and uPA in LLC cells were considerably reduced by α-carotene (0.5, 1, 2.5 μM; 24 hours) in a concentration-dependent manner [2]. In a dose- and time-dependent way, α-Carotene (2, 5, 10 μM; 7 days) suppresses the growth of the human neuroblastoma cell line GOTO. α-Carotene (5 μM; 48 hours) inhibits the proto-oncogene N-Myc's mRNA expression and stops the cell cycle in the G0/G1 phase [3].
α-Carotene (0.5-2.5 μM, 24 h) significantly upregulates TIMP-1 and TIMP-2 protein expression in LLC cells. It inhibits LLC cell invasion (0.5-2.5 μM, 48 h) and reduces MMP-9, MMP-2, and uPA activity. It inhibits GOTO cell proliferation (2-10 μM, 7 days) and induces G0/G1 arrest. |
| ln Vivo |
Alpha-carotene alone (5 mg/kg; oral; twice weekly; for 3 weeks) decreased lung metastases markedly without influencing the growth of the original tumor [2].
α-Carotene (5 mg/kg, oral, twice weekly for 3 weeks) effectively inhibits lung metastasis without affecting primary tumor growth. In vivo tumor reduction has been observed in models where β-carotene was inactive. It suppresses liver and lung carcinogenesis more effectively than β-carotene. |
| Enzyme Assay |
Enzyme activity assays are performed to measure the effects of α-Carotene on MMP-9, MMP-2, and uPA activity. Cell invasion assays are conducted using LLC cells. Proliferation assays are performed using GOTO neuroblastoma cells.
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| Cell Assay |
Western Blot Analysis [2]
Cell Types: Lewis Lung Cancer (LLC) Cell Tested Concentrations: 0.5, 1, 2.5 μM Incubation Duration: 24 hrs (hours) Experimental Results: TIMP-1 and TIMP-2 protein expression Dramatically increased in LLC cells in a concentration-dependent manner. Cell-based assays are conducted using LLC cells to assess invasion and protein expression. GOTO human neuroblastoma cells are used to evaluate proliferation and cell cycle effects. TIMP-1, TIMP-2, and PAI-1 protein levels are measured by Western blot. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 male mice (4 weeks old; 20-25 g) with LLC cells [2]
Doses: 5 mg/kg Route of Administration: Oral; twice weekly; additional 3 weeks Experimental Results: Pulmonary Transfer is Dramatically diminished. In vivo studies are performed in mouse models. α-Carotene (5 mg/kg, oral, twice weekly for 3 weeks) inhibits lung metastasis. It suppresses spontaneous liver carcinogenesis and the promoting stage of lung and skin carcinogenesis in mice. |
| ADME/Pharmacokinetics |
α-Carotene has a molecular weight of 536.87 and a molecular formula of C40H56. It is slightly soluble in DMSO (0.7 mg/mL). Storage: powder at -20°C for up to 3 years; in solvent at -80°C for up to 1 year. Density: 1.00 g/cm³.
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| Toxicity/Toxicokinetics |
α-Carotene is a natural product and is generally considered safe at dietary levels. As a research compound, standard laboratory safety precautions should be followed. It is not intended for human therapeutic use.
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| References |
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| Additional Infomation |
(6'R)-β,ε-carotene is an α-carotene, and it is the enantiomer of (6'S)-β,ε-carotene. α-Carotene has been reported to be found in sea anemones (Alhagi persarum), tricolor clams (Corbicula sandai), and other organisms with relevant data. Carotene is a general term for a class of pigments found in green, yellow, and leafy vegetables, as well as yellow fruits. These pigments are fat-soluble unsaturated fatty hydrocarbons that function as provitamins and are converted into vitamin A in the intestinal wall through an enzymatic process.
α-Carotene is a natural carotenoid and vitamin A precursor with antioxidant and anti-cancer properties. It is used as an anti-metastatic agent or as an adjuvant for anti-cancer drugs. Synonyms include α-胡萝卜素. |
| Molecular Formula |
C₄₀H₅₆
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|---|---|
| Molecular Weight |
536.87
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| Exact Mass |
536.438
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| CAS # |
7488-99-5
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| PubChem CID |
6419725
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| Appearance |
Reddish brown to red solid powder
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| Density |
0.9±0.1 g/cm3
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| Boiling Point |
644.9±35.0 °C at 760 mmHg
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| Melting Point |
185ºC
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| Flash Point |
341.2±20.8 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.563
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| LogP |
15.45
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
0
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
40
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| Complexity |
1200
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=C(C(CCC1)(C)C)/C=C/C(=C/C=C/C(=C/C=C/C=C(\C)/C=C/C=C(\C)/C=C/[C@H]2C(=CCCC2(C)C)C)/C)/C
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| InChi Key |
ANVAOWXLWRTKGA-NTXLUARGSA-N
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| InChi Code |
InChI=1S/C40H56/c1-31(19-13-21-33(3)25-27-37-35(5)23-15-29-39(37,7)8)17-11-12-18-32(2)20-14-22-34(4)26-28-38-36(6)24-16-30-40(38,9)10/h11-14,17-23,25-28,37H,15-16,24,29-30H2,1-10H3/b12-11+,19-13+,20-14+,27-25+,28-26+,31-17+,32-18+,33-21+,34-22+/t37-/m0/s1
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| Chemical Name |
1,3,3-trimethyl-2-[(1E,3E,5E,7E,9E,11E,13E,15E,17E)-3,7,12,16-tetramethyl-18-[(1R)-2,6,6-trimethylcyclohex-2-en-1-yl]octadeca-1,3,5,7,9,11,13,15,17-nonaenyl]cyclohexene
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| Synonyms |
αCarotene α Carotene
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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 | 1.8626 mL | 9.3132 mL | 18.6265 mL | |
| 5 mM | 0.3725 mL | 1.8626 mL | 3.7253 mL | |
| 10 mM | 0.1863 mL | 0.9313 mL | 1.8626 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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