| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Taspine targets multiple pathways: it inhibits phospholipase A2 (PLA2) and 5-lipoxygenase, suppresses P2X4 receptor activity via PI3K inhibition, acts as an AChE inhibitor, and modulates the EGFR signaling pathway (Erk1/2 and Akt).
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|---|---|
| ln Vitro |
Taspine inhibits growth and induces apoptosis of HUVECs and various cancer cells in a dose-dependent manner. It downregulates VEGF expression, inhibits proliferation and migration of endothelial cells through PI3K and MAPK signaling, and exhibits cytotoxic and antitumor activity.
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| ln Vivo |
Taspine suppresses tumor-induced angiogenesis and shows anti-angiogenic activity. Oral or intraperitoneal administration in rodent models reduces tumor growth and vascularization, with meaningful in vivo activity against various cancers and anti-inflammatory effects in animal models.
|
| Enzyme Assay |
This assay is performed using cell-free systems. Purified enzymes (PLA2, AChE, COX-2) are incubated with varying concentrations of Taspine. Enzyme activity is measured spectrophotometrically via substrate conversion (e.g., arachidonic acid for PLA2, acetylcholine for AChE) to determine IC50 values.
|
| Cell Assay |
HUVECs or cancer cell lines are treated with Taspine (1-100 uM) for 24-72 hours. Cell viability is measured via MTT assay, apoptosis by flow cytometry, and migration by scratch wound assay. VEGF expression is quantified by Western blot or ELISA.
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| Animal Protocol |
A murine tumor xenograft model is used. Mice receive Taspine (5-20 mg/kg) via intraperitoneal or oral administration daily for 2-4 weeks. Tumor volume, weight, microvessel density (CD31 staining), and metastatic nodules are assessed post-treatment.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Taspine are limited. Based on structural similarity to other alkaloids, it is expected to have moderate oral bioavailability and distribute widely across tissues. Further detailed PK studies are needed.
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| Toxicity/Toxicokinetics |
Toxicity data for Taspine are limited but indicate manageable safety at therapeutic doses. Preclinical studies show dose-dependent toxicity at higher doses. Standard safety protocols for alkaloid compounds should be followed during handling.
|
| References | |
| Additional Infomation |
Taspine has reportedly been found in Gymnospermium albertii, Caulophyllum thalictroides, and other organisms with available data.
This is a research-grade natural product, not an approved drug. It shows bacteriostatic and cytotoxic properties and acts as a COX-2 inhibitor. Molecular formula: C20H19NO6; molecular weight: 369.37. It is also known as Thaspine and is used in medicinal chemistry optimization for cancer and inflammation. Purity: ≥98%. |
| Molecular Formula |
C20H19NO6
|
|---|---|
| Molecular Weight |
369.36796
|
| Exact Mass |
369.121
|
| CAS # |
602-07-3
|
| PubChem CID |
215159
|
| Appearance |
White to off-white solid powder
|
| Density |
1.35g/cm3
|
| Boiling Point |
569.6ºC at 760 mmHg
|
| Melting Point |
>300ºC (dec.)
|
| Flash Point |
298.3ºC
|
| Index of Refraction |
1.62
|
| LogP |
2.611
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
27
|
| Complexity |
595
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
MTAWKURMWOXCEO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H19NO6/c1-21(2)8-7-10-9-13(25-4)18-16-14(10)20(23)27-17-12(24-3)6-5-11(15(16)17)19(22)26-18/h5-6,9H,7-8H2,1-4H3
|
| Chemical Name |
5-[2-(dimethylamino)ethyl]-7,14-dimethoxy-2,9-dioxatetracyclo[6.6.2.04,16.011,15]hexadeca-1(14),4(16),5,7,11(15),12-hexaene-3,10-dione
|
| 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
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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 | 2.7073 mL | 13.5366 mL | 27.0731 mL | |
| 5 mM | 0.5415 mL | 2.7073 mL | 5.4146 mL | |
| 10 mM | 0.2707 mL | 1.3537 mL | 2.7073 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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