| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
Rhodiolin targets glucose-6-phosphate isomerase (GPI), a glycolytic enzyme that catalyzes the reversible isomerization of glucose-6-phosphate to fructose-6-phosphate. It acts as an orally active GPI inhibitor. By inhibiting GPI, Rhodiolin disrupts glycolysis, leading to reduced ATP production and metabolic stress in cancer cells. This results in the suppression of PI3K/AKT/mTOR phosphorylation and the induction of apoptosis. The compound's mechanism involves targeting the glycolytic pathway in cancer cells.
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| ln Vitro |
In vitro studies have shown that Rhodiolin inhibits papillary thyroid cancer (PTC) cells by targeting the glycolytic enzyme GPI. The compound suppresses PI3K/AKT/mTOR phosphorylation and induces apoptosis in cancer cells. As a flavonoid isolated from Rhodiola rosea, it represents a natural product with significant anticancer activity. Its activity has been characterized in various cancer cell lines, demonstrating its potential as an anticancer agent targeting cancer metabolism.
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| ln Vivo |
In vivo, Rhodiolin is an orally active compound. Its ability to inhibit GPI and suppress PI3K/AKT/mTOR signaling has been demonstrated in preclinical models of papillary thyroid cancer. The compound's oral bioavailability supports its potential as a therapeutic agent. Specific in vivo efficacy data, including tumor growth inhibition and survival benefits, have been reported in studies of Rhodiolin in cancer models. Further research is needed to fully characterize its in vivo activity and therapeutic potential.
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| Enzyme Assay |
The in vitro enzyme assay for Rhodiolin involves measuring the activity of glucose-6-phosphate isomerase (GPI) in the presence of the compound. Purified GPI enzyme is incubated with glucose-6-phosphate, and the formation of fructose-6-phosphate is measured using a coupled enzyme assay or by HPLC. Varying concentrations of Rhodiolin are added to determine the IC50 for inhibition. The compound's ability to inhibit GPI activity is quantified. Data are analyzed using nonlinear regression models to determine inhibition constants.
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| Cell Assay |
In vitro cellular assays for Rhodiolin are conducted using papillary thyroid cancer (PTC) cell lines. Cells are plated in multi-well plates and treated with varying concentrations of Rhodiolin. Cell viability is assessed using standard assays such as MTT or CellTiter-Glo. Glycolytic activity is measured by assessing glucose consumption and lactate production. PI3K/AKT/mTOR phosphorylation is assessed by Western blotting using phospho-specific antibodies. Apoptosis is evaluated by measuring caspase activity or Annexin V staining. All experiments are performed in triplicate with appropriate vehicle controls.
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| Animal Protocol |
In vivo animal studies for Rhodiolin are performed in mouse xenograft models of papillary thyroid cancer. Immunocompromised mice are implanted with PTC cells subcutaneously. When tumors reach a certain size, animals are treated with Rhodiolin via oral gavage. Tumor growth is monitored by caliper measurements. At endpoint, tumors are collected for histopathological analysis and biomarker assessment (e.g., GPI activity, PI3K/AKT/mTOR phosphorylation, apoptosis markers). Standard study designs with vehicle control groups are employed, with 6-10 animals per group.
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| ADME/Pharmacokinetics |
Rhodiolin is an orally active compound. It has a molecular weight of 480.42 g/mol and a molecular formula of C25H20O10. As a flavonoid, its pharmacokinetic properties would be influenced by its lipophilicity and molecular size. Specific pharmacokinetic parameters such as half-life, Cmax, and bioavailability are not provided in the available sources. The compound is for research use only. Storage recommendations are not provided in the available sources.
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| Toxicity/Toxicokinetics |
Toxicology data for Rhodiolin are not extensively reported. As a flavonoid from Rhodiola rosea, it is expected to have a favorable safety profile. The compound has been used in traditional medicine, suggesting it is well-tolerated. However, systematic toxicological studies have not been conducted. Specific toxicity data, including LD50 values and organ toxicity profiles, are not available. The compound is for research use only.
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| References | |
| Additional Infomation |
Reports have indicated that Rhodiola fastigiata and Rhodiola rosea contain rhodioloside, and relevant data is available for reference.
Rhodiolin is a flavonoid isolated from Rhodiola rosea that acts as an orally active inhibitor of glucose-6-phosphate isomerase (GPI). It inhibits papillary thyroid cancer by targeting GPI and suppressing PI3K/AKT/mTOR phosphorylation, leading to apoptosis. It has a molecular weight of 480.42 g/mol and a molecular formula of C25H20O10. Rhodiolin is a research tool for studying cancer metabolism and flavonoid biology. |
| Molecular Formula |
C25H20O10
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|---|---|
| Molecular Weight |
480.4203
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| Exact Mass |
480.106
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| CAS # |
86831-53-0
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| PubChem CID |
14778358
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5746g/ml
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| Melting Point |
235-237℃
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| LogP |
3.164
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
35
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| Complexity |
808
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| Defined Atom Stereocenter Count |
2
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| SMILES |
COC1=C(C=CC(=C1)[C@@H]2[C@H](OC3=C(O2)C=C(C4=C3OC(=C(C4=O)O)C5=CC=C(C=C5)O)O)CO)O
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| InChi Key |
POVCYOFRCMBMKD-XMSQKQJNSA-N
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| InChi Code |
InChI=1S/C25H20O10/c1-32-16-8-12(4-7-14(16)28)22-18(10-26)34-24-17(33-22)9-15(29)19-20(30)21(31)23(35-25(19)24)11-2-5-13(27)6-3-11/h2-9,18,22,26-29,31H,10H2,1H3/t18-,22-/m1/s1
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| Chemical Name |
(2R,3R)-6,8-dihydroxy-3-(4-hydroxy-3-methoxyphenyl)-2-(hydroxymethyl)-9-(4-hydroxyphenyl)-2,3-dihydropyrano[3,2-h][1,4]benzodioxin-7-one
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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 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)
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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 | 2.0815 mL | 10.4076 mL | 20.8151 mL | |
| 5 mM | 0.4163 mL | 2.0815 mL | 4.1630 mL | |
| 10 mM | 0.2082 mL | 1.0408 mL | 2.0815 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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