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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. |
| References | |
| Additional Infomation |
Bufalin is a 14beta-hydroxy steroid that is bufan-20,22-dienolide having hydroxy substituents at the 5beta- and 14beta-positions. It has been isolated from the skin of the toad Bufo bufo. It has a role as an antineoplastic agent, a cardiotonic drug, an anti-inflammatory agent and an animal metabolite. It is a 3beta-hydroxy steroid and a 14beta-hydroxy steroid. It is functionally related to a bufanolide.
Bufalin has been reported in Phrynoidis asper, Bufo gargarizans, and other organisms with data available. Bufalin is an active ingredient and one of the glycosides in the traditional Chinese medicine ChanSu; it is also a bufadienolide toxin originally isolated from the venom of the Chinese toad Bufo gargarizans, with potential cardiotonic and antineoplastic activity. Although the mechanism of action of bufalin is still under investigation, this agent is a specific Na+/K+-ATPase inhibitor and can induce apoptosis in cancer cell lines through the activation of the transcription factor AP-1 via a mitogen activated protein kinase (MAPK) pathway. |
| Molecular Formula |
C24H34O4
|
|---|---|
| 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
|
| 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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