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Chemical Structure| 465-39-4 Chemical Structure| 465-39-4

Structure of Resibufogenin
CAS No.: 465-39-4

Chemical Structure| 465-39-4

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Resibufogenin, a natural product isolated and purified from the glandular body of Bufo bufo gargarizans Cantor, displays great potential as a chemotherapeutic agent in oncology.

Synonyms: Bufogenin; Recibufogenin; Bufotenine

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Product Details of Resibufogenin

CAS No. :465-39-4
Formula : C24H32O4
M.W : 384.51
SMILES Code : C[C@]([C@@H](C(C=C1)=COC1=O)C2)(CC[C@@]3([H])[C@@]4([H])CC[C@@]5([H])[C@@]3(CC[C@H](O)C5)C)[C@@]64[C@@H]2O6
Synonyms :
Bufogenin; Recibufogenin; Bufotenine
MDL No. :MFCD00210361

Safety of Resibufogenin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Resibufogenin

MAPK
PI3K-AKT
pyroptosis
Hedgehog

Isoform Comparison

Biological Activity

Target
  • PI3K

In Vitro:

Cell Line
Concentration Treated Time Description References
Human renal cancer cell Caki-1 10 nM, 50 nM, 100 nM, 200 nM 12 h and 24 h Resibufogenin significantly inhibited the proliferation and migration of Caki-1 cells and induced apoptosis and necrosis in a dose-dependent manner. Biology (Basel). 2024 Dec 19;13(12):1064.
HepG2 cells 1.25, 2.5, 5.0, 10.0, and 20.0 μg/mL 24, 48, and 72 h To assess the in vitro cytotoxicity of nanoparticles on HepG2 cells. The results showed that the RGPPN group exhibited higher toxic effects than the RPN, RPPN, and RGP&PN groups, which was consistent with the fluorescence intensity and RBG content in the cellular uptake test. Drug Deliv. 2017 Nov;24(1):1302-1316.
RIP3+/+ and RIP3−/− mouse embryo fibroblasts (MEF) 10 and 20 μM 24 h To evaluate whether Resibufogenin-induced necrotic death is RIP3-dependent, results showed that RIP3−/− cells had higher viability than wild-type cells. J Transl Med. 2018 Jul 20;16(1):201.
HCT-116 cells 0.1, 1, 2.5, 5, 10 μM 24–48 h To evaluate the anti-proliferative activity of Resibufogenin on CRC cells, results showed that Resibufogenin dose-dependently reduced cell viability. J Transl Med. 2018 Jul 20;16(1):201.
SW480 cells 0.1, 1, 2.5, 5, 10 μM 24–48 h To evaluate the anti-proliferative activity of Resibufogenin on CRC cells, results showed that Resibufogenin dose-dependently reduced cell viability. J Transl Med. 2018 Jul 20;16(1):201.
HPDE cells 58.12 μM (IC50) 48 h To evaluate the cytotoxicity of RB on normal pancreatic epithelial cells HPDE, results showed that RB displayed selective cytotoxicity against tumor cells. Cancer Sci. 2018 Nov;109(11):3611-3622.
Aspc cells 4.76 μM (IC50) 48 h To evaluate the effect of RB on Aspc cell viability, results showed that RB significantly inhibited cell growth in a concentration- and time-dependent manner. Cancer Sci. 2018 Nov;109(11):3611-3622.
Panc-1 cells 2.88 μM (IC50) 48 h To evaluate the effect of RB on Panc-1 cell viability, results showed that RB significantly inhibited cell growth in a concentration- and time-dependent manner. Cancer Sci. 2018 Nov;109(11):3611-3622.
Human umbilical vein endothelial cells (HUVECs) 1, 3 μM 24 h To evaluate the effect of RBF on spheroid sprouting of HUVECs, results showed that RBF significantly inhibited the spheroid sprouting ability of HUVECs. Front Pharmacol. 2021 Apr 30;12:682735.
Human umbilical vein endothelial cells (HUVECs) 0.3, 1, 3, 10 μM 10 h To evaluate the effect of RBF on tube formation of HUVECs, results showed that RBF significantly inhibited the tube formation ability of HUVECs. Front Pharmacol. 2021 Apr 30;12:682735.
Human umbilical vein endothelial cells (HUVECs) 0.3, 1, 3, 10, 30 μM 24 h To evaluate the effect of RBF on the viability of HUVECs, results showed that RBF inhibited the cell viability of HUVECs in a dose-dependent manner with an IC50 value of 3 μM. Front Pharmacol. 2021 Apr 30;12:682735.
A172 cells 6.21 μM (IC50) 48 h RB significantly inhibited GBM cell proliferation and induced G2/M phase arrest Front Pharmacol. 2022 May 17;13:855626.
U251 cells 3.05 μM (IC50) 48 h RB significantly inhibited GBM cell proliferation and induced G2/M phase arrest Front Pharmacol. 2022 May 17;13:855626.
P3#GBM cells 2.29 μM (IC50) 48 h RB significantly inhibited GBM cell proliferation and induced G2/M phase arrest Front Pharmacol. 2022 May 17;13:855626.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c-nu mice Heterotropic CRC tumor model Intraperitoneal injection 5 and 10 mg/kg Once daily for 21 days To evaluate the inhibitory effect of Resibufogenin on CRC tumor growth, results showed that Resibufogenin dose-dependently reduced tumor volume and weight. J Transl Med. 2018 Jul 20;16(1):201.
BALB/c nude mice Aspc xenograft model Intragastric injection 10 mg/kg and 20 mg/kg Once daily for 20 days To evaluate the inhibitory effect of RB on Aspc xenograft tumor growth, results showed that RB significantly suppressed tumor growth without systemic toxicity. Cancer Sci. 2018 Nov;109(11):3611-3622.
C57BL/6 mice Matrigel plug model Subcutaneous injection 10, 30 μM 7 days To evaluate the antiangiogenic effect of RBF in vivo, results showed that RBF significantly inhibited VEGF-stimulated angiogenesis. Front Pharmacol. 2021 Apr 30;12:682735.
BALB/c nude mice Orthotopic xenograft model Intraperitoneal injection 10 mg/kg Daily until the end of the experiment RB significantly inhibited tumor growth and prolonged the median survival of tumor-bearing mice Front Pharmacol. 2022 May 17;13:855626.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.00mL

2.60mL

1.30mL

26.01mL

5.20mL

2.60mL

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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