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Chemical Structure| 465-21-4 Chemical Structure| 465-21-4

Structure of Bufalin
CAS No.: 465-21-4

Chemical Structure| 465-21-4

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Bufalin a major digoxin-like immunoreactive component of the Chinese medicine Chan Su and has been shown to exert a potential for anticancer activity against various human cancer cell lines in vitro.

Synonyms: NSC 89595; BF

4.5 *For Research Use Only !

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Product Details of Bufalin

CAS No. :465-21-4
Formula : C24H34O4
M.W : 386.52
SMILES Code : O=C(C=C1)OC=C1[C@H]2CC[C@]3(O)[C@]4([H])CC[C@]5([H])C[C@@H](O)CC[C@]5(C)[C@@]4([H])CC[C@@]32C
Synonyms :
NSC 89595; BF
MDL No. :MFCD00056525

Safety of Bufalin

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H300
Precautionary Statements:P264-P270-P301+P310+P330-P405-P501
Class:6.1
UN#:3462
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
SK-N-BE(2) 90 nM 72 hours Inhibits cell proliferation and migration Int J Mol Med. 2020 Dec;46(6):2137-2149.
SH-SY5Y 30 nM 72 hours Inhibits cell proliferation and migration Int J Mol Med. 2020 Dec;46(6):2137-2149.
Vero cells 0.0625 µM, 0.125 µM, 0.25 µM, 0.5 µM, 1 µM 24 hours To evaluate the inhibitory effect of Bufalin on HSV-1 replication, results showed Bufalin significantly inhibited HSV-1 replication. Int J Mol Sci. 2023 Sep 23;24(19):14479.
PK-15 cells 0.015 µM, 0.03 µM, 0.06 µM, 0.12 µM 24 hours To evaluate the inhibitory effect of Bufalin on PRV replication, results showed Bufalin significantly inhibited PRV replication. Int J Mol Sci. 2023 Sep 23;24(19):14479.
Human umbilical vein endothelial cells (HUVECs) 10 nM 24 hours To evaluate the effect of Bufalin on TME-mediated angiogenesis, results showed that Bufalin significantly inhibited HUVEC tube formation, migration, and adhesion induced by TME cells. J Transl Med. 2021 Sep 8;19(1):383.
L02 0, 20, 40, 80, 160, 320 nM 24, 48, 72 hours Bufalin had no significant inhibitory effect on normal hepatocyte L02 cells. J Transl Med. 2023 Dec 11;21(1):900.
RBE 0, 20, 40, 80, 160, 320 nM 24, 48, 72 hours Bufalin significantly inhibited the proliferation and migration of RBE cells in a dose- and time-dependent manner. J Transl Med. 2023 Dec 11;21(1):900.
QBC-939 0, 20, 40, 80, 160, 320 nM 24, 48, 72 hours Bufalin significantly inhibited the proliferation and migration of QBC-939 cells in a dose- and time-dependent manner. J Transl Med. 2023 Dec 11;21(1):900.
HCCC-9810 0, 20, 40, 80, 160, 320 nM 24, 48, 72 hours Bufalin significantly inhibited the proliferation and migration of HCCC-9810 cells in a dose- and time-dependent manner. J Transl Med. 2023 Dec 11;21(1):900.
U266R 24 nM 48 hours Bufalin alone increased p-AKT levels in U266R cells, and combination with MK2206 enhanced apoptosis induction. Cell Death Dis. 2017 May 11;8(5):e2776.
H929R 24 nM 48 hours Bufalin alone increased p-AKT levels in H929R and U266R cells, and combination with MK2206 enhanced apoptosis induction. Cell Death Dis. 2017 May 11;8(5):e2776.
U266 12 nM 48 hours Bufalin alone moderately induced apoptosis in U266 cells, accompanied by increased p-AKT levels. Cell Death Dis. 2017 May 11;8(5):e2776.
NCI-H929 12 nM 48 hours Bufalin alone moderately induced apoptosis in H929 and U266 cells, accompanied by increased p-AKT levels. Cell Death Dis. 2017 May 11;8(5):e2776.
HepG2 cells 5, 10, 20 or 50 nM 48 hours To evaluate the effects of Bufalin on proliferation and apoptosis of HepG2 cells. Bufalin at higher concentrations could inhibit proliferation and induce apoptosis of HepG2 cells. Oncoimmunology. 2018 Feb 8;7(5):e1426434.
MHCC97 H cells 5, 10, 20 or 50 nM 48 hours To evaluate the effects of Bufalin on proliferation and apoptosis of HCC cells. Bufalin (higher than 10 nM) could inhibit cell proliferation and induce apoptosis of HCC cells. Oncoimmunology. 2018 Feb 8;7(5):e1426434.
CEF cells 0.0625 µM, 0.125 µM, 0.25 µM, 0.5 µM, 1 µM 48 hours To evaluate the inhibitory effect of Bufalin on MDV replication, results showed Bufalin significantly inhibited MDV replication. Int J Mol Sci. 2023 Sep 23;24(19):14479.
Recombinant human CYP3A4 0, 0.1, 0.5, 1, 2.5, 5, 7.5, 10, 15, 20, 30 µM 5 minutes To determine the inhibitory effect of Bufalin on CYP3A4 activity, the IC50 value was 14.52 μmol/L. Acta Pharmacol Sin. 2009 May;30(5):646-52.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice PRV infection model Intraperitoneal injection 0.5 mg/kg Every 36 hours until all mice in the PRV-infected group had died To evaluate the therapeutic effect of Bufalin on PRV infection, results showed Bufalin significantly decreased the viral load in multiple tissues and increased the survival rate of mice. Int J Mol Sci. 2023 Sep 23;24(19):14479.
Balb/c nu/nu mice HCC xenograft model Intraperitoneal injection 0.5, 1 or 2 mg/kg Once a week (poly (I:C)) or five days a week (bufalin) for six weeks To evaluate the effects of Bufalin on lung metastasis in HCC xenograft model. Bufalin (0.5 mg/kg) could inhibit poly (I:C)-enhanced lung metastasis of HCC cells. Oncoimmunology. 2018 Feb 8;7(5):e1426434.
BALB/c nu/nu mice MOPC315 xenograft model Intraperitoneal injection 1 mg/kg Once daily for 10 days Combination treatment significantly inhibited MM tumor growth without significant side effects. Cell Death Dis. 2017 May 11;8(5):e2776.
BALB/c nude mice ICC xenograft model Intraperitoneal injection 1 mg/kg Every two days for 2-3 weeks Bufalin significantly inhibited CAMKK2 overexpression-induced ICC tumor growth. J Transl Med. 2023 Dec 11;21(1):900.
BALB/c mice Subcutaneous xenograft tumor model and liver metastasis model Intraperitoneal injection 1 mg/kg Once every other day for 21 days (flank) or 14 days (spleen) To evaluate the antiangiogenic activity of Bufalin in vivo, results showed that Bufalin significantly inhibited tumor growth and liver metastasis, reducing the number of tumor blood vessels and STAT3 phosphorylation in vascular endothelial cells. J Transl Med. 2021 Sep 8;19(1):383.
SCID/NOD mice MM xenograft model Intraperitoneal injection 1 mg/kg Twice weekly AHSA1 overexpression promotes MM cell growth and BTZ resistance J Exp Clin Cancer Res. 2022 Jan 6;41(1):11
Wistar rats Healthy male Wistar rats Oral (ig) and intravenous (iv) injection 10 mg/kg Single dose To evaluate the effect of Bufalin on CYP3A4 activity, results showed that Bufalin significantly increased AUC0–t and t1/2, and decreased CL and the formation of 1-hydroxy-midazolam. Acta Pharmacol Sin. 2009 May;30(5):646-52.
C57BL/6 mice Orthotopic HCC model Intraperitoneal injection 10 μg/kg Every other day for 3 weeks To investigate the inhibitory effect of bufalin on HCC in immunocompetent mice, results showed that bufalin promoted macrophage polarization toward M1 phenotype, activated antitumor T cell immune response, and thereby suppressed HCC growth. J Immunother Cancer. 2022 May;10(5):e004297
BALB/c nude mice 4T1 breast cancer model Intravenous injection 2 mg/kg Every 2 days for 3 weeks Evaluate the in vivo antitumor efficacy of FA-MOF/Buf NPs, showing significant tumor growth inhibition and reduced side effects. Front Pharmacol. 2022 Jan 18;12:747992
Nude mice Subcutaneous xenograft model Intraperitoneal injection 5 mg/kg Three times per week for 4 weeks Inhibits tumor growth Int J Mol Med. 2020 Dec;46(6):2137-2149.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.94mL

2.59mL

1.29mL

25.87mL

5.17mL

2.59mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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