| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| ln Vitro |
Conobafagin (30–300 nM, 24 hours) stimulates OCM1 cells to exhibit and exhibit associated changes in surface activity while inhibiting the G1 phase of the cell cycle in a concentration-inhibitory manner [1]. In uveal melanoma OCM1 cells, conobafagin (30-300 nM, 7 days) exhibits strong anticancer activity in a dose-dependent manner [1]. In pleomorphic astroblastoma U87MG-EGFR and U87MG-PTEN cells, conobafagin (0.01-1 μM, 6 hours) burns growth factor receptor (EGFR) phosphorylation, causing cellular anemia and cytotoxicity [2]. Cinobupsin (0.4, 0.7, 1.0 μM, 24-48 hours) initiates the G2/M phase of the cell life cycle, which results in
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| ln Vivo |
In an induced xenograft model, cinobufonin (5 mg/kg intraperitoneally, once day for 10 days) inhibits cytochromes, hence suppressing xenograft growth [1]. In subcutaneous and intracranial U87MG-EGFR xenograft mouse models, cinobufen (5 mg/kg intraperitoneally, once day for 10 days) slows tumor growth and increases the median survival of nude mice with intracranial U87MGEGFR tumors. rate [2].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: OCM1 cell Tested Concentrations: 30,100,300 nM Incubation Duration: 7 days Experimental Results: Yes OCM1 cells produced potent cytotoxicity with an IC50 of 8.023 nM. Apoptosis analysis[1] Cell Types: OCM1 Cell Tested Concentrations: 30,100,300 nM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of apoptosis and upregulation of cleaved caspase-3, cleaved poly(ADP-ribose) polymerase (PARP) and cleaved caspase Expression level -9. Activation of the intrinsic mitochondrial apoptotic pathway, manifested by increased apoptosis, increased expression of Bad and Bax, diminished expression of Bcl-2 and Bcl-xl, and diminished mitochondrial membrane potential (MMP). |
| Animal Protocol |
Animal/Disease Models: OCM1 cell tumor Nu/Nu nude mouse xenograft [1]
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection, one time/day for 10 days. Experimental Results: The tumor growth rate is higher than that of intraperitoneal (ip) injection of normal saline or no Treated tumors grow more slowly. The expression of caspase-3 and PARP increased in tumor tissue, the expression of Bcl-2 and Bcl-xl diminished, and the expression of Bad and Bax increased in mouse tumor tissue. Animal/Disease Models: U87MG-EGFR subcutaneousand intracranial xenograft model [2] Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection, one time/day for 10 days. Experimental Results: The luminescence intensity of brain tumors diminished by approximately 70%. Levels of p-EGFR, p-STAT3, and p-Akt were diminished in intracranial tumors compared with vehicle. Intracranial tumors had diminished immunostaining for Ki67 and active caspase-3. |
| References |
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| Additional Infomation |
Cinobufagin is a steroid lactone. It is functionally related to a bufanolide.
Cinobufagin has been reported in Phrynoidis asper, Bufo gargarizans, and other organisms with data available. Cinobufagin is a bufadienolide compound extracted from the dried venom secreted by the parotid glands of toads and one of the glycosides in the traditional Chinese medicine ChanSu, with potential antineoplastic activity. Although the mechanism of action of cinobufagin is still under investigation, it has been found to suppress cancer cell proliferation and cause apoptosis in cancer cells via a sequence of apoptotic modulators that include mitochondrial Bax and cytosolic chromosome c, and caspases 3, 8, and 9. Possible upstream mediators of cinobufagin-induced apoptosis include Fas and p53. |
| Molecular Formula |
C26H34O6
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|---|---|
| Molecular Weight |
442.552
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| Exact Mass |
442.235
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| CAS # |
470-37-1
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| PubChem CID |
11969542
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
595.4±50.0 °C at 760 mmHg
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| Melting Point |
222-223ºC
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| Flash Point |
199.4±23.6 °C
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| Vapour Pressure |
0.0±3.8 mmHg at 25°C
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| Index of Refraction |
1.595
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| LogP |
2.43
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
32
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| Complexity |
923
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| Defined Atom Stereocenter Count |
10
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| SMILES |
CC(=O)O[C@@H]1[C@@H]([C@]2(CC[C@H]3[C@H]([C@@]24[C@@H]1O4)CC[C@H]5[C@@]3(CC[C@@H](C5)O)C)C)C6=COC(=O)C=C6
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| InChi Key |
SCULJPGYOQQXTK-OLRINKBESA-N
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| InChi Code |
InChI=1S/C26H34O6/c1-14(27)31-22-21(15-4-7-20(29)30-13-15)25(3)11-9-18-19(26(25)23(22)32-26)6-5-16-12-17(28)8-10-24(16,18)2/h4,7,13,16-19,21-23,28H,5-6,8-12H2,1-3H3/t16-,17+,18+,19-,21+,22-,23-,24+,25-,26-/m1/s1
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| Chemical Name |
[(1R,2S,4R,5R,6R,7R,10S,11S,14S,16R)-14-hydroxy-7,11-dimethyl-6-(6-oxopyran-3-yl)-3-oxapentacyclo[8.8.0.02,4.02,7.011,16]octadecan-5-yl] acetate
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| Synonyms |
NSC90325 14,15β-Epoxy-3β,16β-dihydroxy-5β,20(22)-bufadienolide 16-acetateCinobufagine Cino-bufaginCinobufagin
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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) |
DMSO : ≥ 100 mg/mL (~225.97 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.65 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.65 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.65 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2596 mL | 11.2982 mL | 22.5963 mL | |
| 5 mM | 0.4519 mL | 2.2596 mL | 4.5193 mL | |
| 10 mM | 0.2260 mL | 1.1298 mL | 2.2596 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01236690 | UNKNOWN STATUS | Drug: Cinobufacin injection | Cinobufacin Injection Hepatoma |
Changhai Hospital | 2010-11 | Phase 2 |
| NCT03843229 | UNKNOWN STATUS | Drug: Cinobufacini injection Procedure: Transarterial Chemoembolization(TACE) Drug: cinobufacini tablet |
Liver Cancer | The First Affiliated Hospital of Dalian Medical University | 2019-01-27 | Phase 4 |
| NCT02530398 | UNKNOWN STATUS | Drug: Cinobufacini Injection | Digestive System Cancer Malignant Ascites |
Dongfang Hospital Beijing University of Chinese Medicine | 2015-07 | Phase 1 |
| NCT02860429 | UNKNOWN STATUS | Drug: Cinobufacini injection Drug: chemotherapy |
Gastrointestinal Neoplasms | Xiaonan Cui | 2016-09 | Phase 4 |
| NCT02871869 | UNKNOWN STATUS | Drug: vindesine Drug: cyclophosphamide Drug: Epirubicin |
Diffuse, Large B-Cell, Lymphoma | Xinjiang Medical University | 2016-09 | Phase 2 Phase 3 |
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