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| Targets |
Pseudoginsenoside Rh2 targets the Ras/Raf/ERK/p53 signaling pathway in cancer cells. It induces mitochondrial apoptosis through excessive activation of this pathway. The compound's mechanism involves the activation of the Ras/Raf/ERK cascade, leading to p53 activation and subsequent mitochondrial dysfunction and apoptosis. Pseudoginsenoside Rh2 is a derivative of ginsenoside Rh2 and shares similar biological activities, including cytotoxicity against various cancer cell lines. It also exhibits antioxidative activity in both its (20Z) and (20E) isomers.
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| ln Vitro |
In vitro, pseudoginsenoside Rh2 has cytotoxicity against A549 lung cancer cells. It induces mitochondrial apoptosis in these cells and is responsible for excessive activation of the Ras/Raf/ERK/p53 pathway. The compound's cytotoxic effects are mediated through the mitochondrial apoptosis pathway, leading to cell death. Both (20Z)- and (20E)-pseudoginsenoside Rh2 exhibit antioxidative activity. The compound has potential as an anticancer agent, though specific IC₅₀ values for its cytotoxicity have not been reported in the available literature.
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| ln Vivo |
In vivo activity of pseudoginsenoside Rh2 has not been extensively characterized in animal models. No specific in vivo studies have been reported for this compound. The compound is a novel derivative of ginsenoside Rh2 and has potential anticancer activity. However, the lack of in vivo data limits the current understanding of its efficacy, pharmacokinetics, and safety in animal models. Further studies are needed to evaluate its therapeutic potential in vivo.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for pseudoginsenoside Rh2 have not been extensively developed or reported. The compound's primary reported activity is cytotoxicity against A549 cells and induction of mitochondrial apoptosis through activation of the Ras/Raf/ERK/p53 pathway. These effects are typically assessed in cell-based assays rather than in direct enzyme or receptor binding studies. Further studies are needed to identify the specific molecular targets and binding affinities of pseudoginsenoside Rh2.
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| Cell Assay |
In vitro cell-based assays for pseudoginsenoside Rh2 typically employ A549 lung cancer cells. Cells are cultured in appropriate medium (e.g., RPMI-1640 or DMEM supplemented with fetal bovine serum) and treated with various concentrations of the compound for 24-72 hours. Cell viability is assessed by MTT, CCK-8, or SRB assays to determine cytotoxicity. Apoptosis is evaluated by Annexin V/PI staining and flow cytometry, as well as by detection of caspase-3/7 activation and mitochondrial membrane potential loss using fluorescent dyes. The Ras/Raf/ERK/p53 pathway activation is assessed by Western blot analysis of phosphorylated ERK, Raf, and p53 levels.
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| Animal Protocol |
In vivo animal studies have not been reported for pseudoginsenoside Rh2. No animal models have been used to evaluate its pharmacokinetics, efficacy, or toxicology. The compound is a novel derivative of ginsenoside Rh2 and has potential anticancer activity. Future studies may involve administration of the compound in rodent xenograft models to evaluate its antitumor efficacy. Currently, no in vivo data are available.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of pseudoginsenoside Rh2 have not been characterized. No absorption, distribution, metabolism, or excretion studies have been conducted for this compound. As a ginsenoside derivative, the compound may have limited oral bioavailability and may undergo metabolism in the liver and gastrointestinal tract. However, these properties have not been experimentally determined. Further studies are needed to evaluate the compound's PK profile.
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| Toxicity/Toxicokinetics |
The toxicity profile of pseudoginsenoside Rh2 has not been extensively characterized in preclinical studies. No acute toxicity, genotoxicity, or chronic toxicity studies have been reported. The compound's cytotoxicity against cancer cells suggests potential toxicity to normal cells as well. However, specific toxicology data are not available. The compound is intended for research use only and is not approved for human therapeutic applications.
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| References |
: Qian G, et al. Synthesis and anti-cancer cell activity of pseudo-ginsenoside Rh2. Steroids. 2014 Dec;92:1-6.
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| Additional Infomation |
Pseudoginsenoside Rh2 is a research-grade novel derivative of ginsenoside Rh2. It has a molecular formula of C₃₆H₆₂O₈ and a molecular weight of 622.87. The compound exhibits cytotoxicity and induces mitochondrial apoptosis in A549 lung cancer cells through excessive activation of the Ras/Raf/ERK/p53 pathway. Both (20Z)- and (20E)-pseudoginsenoside Rh2 have antioxidative activity. It is not an approved therapeutic drug and has no clinical trial history. The compound is supplied as a high-purity powder (≥97%) and is intended for research use only.
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| Molecular Formula |
C₃₆H₆₂O₈
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|---|---|
| Molecular Weight |
622.87
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| Exact Mass |
622.444
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| CAS # |
1370264-16-6
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| Related CAS # |
(Z)-Pseudoginsenoside Rh2;1636114-55-0
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| PubChem CID |
101887367
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
726.2±60.0 °C at 760 mmHg
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| Flash Point |
393.0±32.9 °C
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| Vapour Pressure |
0.0±5.4 mmHg at 25°C
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| Index of Refraction |
1.572
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| LogP |
5.35
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
44
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| Complexity |
1070
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| Defined Atom Stereocenter Count |
14
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| SMILES |
O([H])[C@]1([H])C([H])([H])[C@]2([H])[C@@]3(C([H])([H])[H])C([H])([H])C([H])([H])[C@@]([H])(C(C([H])([H])[H])(C([H])([H])[H])[C@]3([H])C([H])([H])C([H])([H])[C@@]2(C([H])([H])[H])[C@]2(C([H])([H])[H])C([H])([H])C([H])([H])[C@]([H])(/C(=C(/[H])\C([H])([H])C([H])([H])C(C([H])([H])[H])(C([H])([H])[H])O[H])/C([H])([H])[H])[C@]21[H])O[C@@]1([H])[C@@]([H])([C@]([H])([C@@]([H])([C@@]([H])(C([H])([H])O[H])O1)O[H])O[H])O[H]
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| InChi Key |
YCDZBVXSGVWFFX-UKHVTAPLSA-N
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| InChi Code |
InChI=1S/C36H62O8/c1-20(10-9-14-32(2,3)42)21-11-16-36(8)27(21)22(38)18-25-34(6)15-13-26(33(4,5)24(34)12-17-35(25,36)7)44-31-30(41)29(40)28(39)23(19-37)43-31/h10,21-31,37-42H,9,11-19H2,1-8H3/b20-10-/t21-,22-,23-,24+,25-,26+,27+,28-,29+,30-,31+,34+,35-,36-/m1/s1
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| Chemical Name |
(2R,3R,4S,5S,6R)-2-[[(3S,5R,8R,9R,10R,12R,13R,14R,17S)-12-hydroxy-17-[(Z)-6-hydroxy-6-methylhept-2-en-2-yl]-4,4,8,10,14-pentamethyl-2,3,5,6,7,9,11,12,13,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl]oxy]-6-(hydroxymethyl)oxane-3,4,5-triol
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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 | 1.6055 mL | 8.0274 mL | 16.0547 mL | |
| 5 mM | 0.3211 mL | 1.6055 mL | 3.2109 mL | |
| 10 mM | 0.1605 mL | 0.8027 mL | 1.6055 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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