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| 10mg |
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Bufalin is a novel and potent inhibitor of steroid receptor coactivator 3 (SRC-3) with anticancer, anti-inflammatory and antinociceptive activity. It is a naturally occurring digoxin-like immunoreactive component isolated from the Chinese medicine Chan Su. It exerts anticancer activity by inducing cell death through the ROS-mediated RIP1/RIP3/PARP-1 pathways.
| ln Vitro |
In NCI-H460 cells, bufalin (0, 1, 2, 4 μM) reduces cell viability for 48 hours[2]. Bufalin (2 μM) decreases the expression of GRP78 mRNA while increasing that of caspae-3, Endo G, and GADD153 mRNA[2].
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|---|---|
| ln Vivo |
Mice harboring NCI-H460 cells demonstrated notable antitumor activity when bufalin (0.1, 0.2, or 0.4 mg/kg, intraperitoneally injected once daily for 14 days) was administered [2].
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| Cell Assay |
Cell viability assay[2]
Cell Types: NCI-H460 Cell Tested Concentrations: 0, 1, 2, 4 μM Incubation Duration: 48 hrs (hours) Experimental Results: The viability of NCI-H460 cells was diminished in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: 40 male athymic BALB/c nu/nu (nude) mice (6-8 weeks old) [2]
Doses: 0.1, 0.2 or 0.4 mg/kg Route of Administration: Daily intraperitoneal (ip) injection until 14 days Experimental Results: Dose dependent Inhibit tumor growth. Male athymic BALB/c nu/nu mice (6–8 weeks old) were acclimated for 7 days. NCI-H460 cells (1×10^7 cells/mouse) were subcutaneously injected into one flank. Tumor size was measured every 3 days using calipers, and tumor volume calculated as V = L × W^2 / 2. When tumor volume exceeded 100 mm^3, mice were randomly divided into four groups (n=10 per group). They received intraperitoneal injections of either vehicle (0.1% DMSO) or bufalin at 0.1, 0.2, or 0.4 mg/kg once daily until day 14 after therapy initiation. At the end of the experiment, animals were anaesthetized with CO2 and sacrificed. Tumors were removed, photographed, measured, and weighed [2] |
| References | |
| Additional Infomation |
Bufalin is a 14β-hydroxy steroid with the structure bufotoxin-20,22-diene lactone, containing hydroxyl substituents at both the 5β- and 14β- positions. It has been isolated from the skin of the toad (Bufo bufo). Bufalin possesses antitumor, cardiotonic, anti-inflammatory, and animal metabolic effects. It is a 3β- and 14β-hydroxy steroid, functionally related to bufotoxin lactone. Bufalin has been reported to exist in the African toad (Phrynoidis asper), the Chinese toad (Bufo gargarizans), and other organisms with relevant data. Bufalin is one of the active ingredients of the traditional Chinese medicine toad venom, and is also a glycoside compound; it was originally isolated from the venom of the Chinese toad (Bufo gargarizans) as a bufodiene lactone toxin, possessing potential cardiotonic and antitumor activities. Although the pharmacological mechanism of bufalin is still under investigation, it is a specific Na+/K+-ATPase inhibitor that can activate transcription factor AP-1 through the mitogen-activated protein kinase (MAPK) pathway, thereby inducing apoptosis in cancer cell lines.
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| Molecular Formula |
C24H34O4
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|---|---|
| Molecular Weight |
386.53
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| Exact Mass |
386.245
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| CAS # |
465-21-4
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| PubChem CID |
9547215
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
556.6±50.0 °C at 760 mmHg
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| Melting Point |
242 - 243ºC
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| Flash Point |
189.0±23.6 °C
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| Vapour Pressure |
0.0±3.4 mmHg at 25°C
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| Index of Refraction |
1.594
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| LogP |
3.42
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
28
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| Complexity |
741
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| Defined Atom Stereocenter Count |
8
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| SMILES |
O([H])[C@]12C([H])([H])C([H])([H])[C@]([H])(C3=C([H])OC(C([H])=C3[H])=O)[C@@]1(C([H])([H])[H])C([H])([H])C([H])([H])[C@]1([H])[C@@]3(C([H])([H])[H])C([H])([H])C([H])([H])[C@@]([H])(C([H])([H])[C@@]3([H])C([H])([H])C([H])([H])[C@@]21[H])O[H]
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| InChi Key |
QEEBRPGZBVVINN-BMPKRDENSA-N
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| InChi Code |
InChI=1S/C24H34O4/c1-22-10-7-17(25)13-16(22)4-5-20-19(22)8-11-23(2)18(9-12-24(20,23)27)15-3-6-21(26)28-14-15/h3,6,14,16-20,25,27H,4-5,7-13H2,1-2H3/t16-,17+,18-,19+,20-,22+,23-,24+/m1/s1
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| Chemical Name |
5-[(3S,5R,8R,9S,10S,13R,14S,17R)-3,14-dihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]pyran-2-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 |
| 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 (~258.72 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.47 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.38 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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5871 mL | 12.9356 mL | 25.8712 mL | |
| 5 mM | 0.5174 mL | 2.5871 mL | 5.1742 mL | |
| 10 mM | 0.2587 mL | 1.2936 mL | 2.5871 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 |
| NCT00837239 | COMPLETED | Drug: Gemcitabine Drug: HuaChanSu Drug: Placebo |
Pancreatic Cancer | M.D. Anderson Cancer Center | 2007-06 | Phase 2 |
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