[CAS NO. 471-95-4]  Bufotalin

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PRODUCTS SPECIFICATIONS [471-95-4]

Catalog
AS985820
Brand
Arctom Scientific
CAS
471-95-4

DESCRIPTION [471-95-4]

Overview

MDL-
Molecular Weight444.56
Molecular FormulaC26H36O6
SMILESC[C@@]1(CC[C@@]2([H])[C@@]3([H])CC[C@@]4([H])[C@@]2(CC[C@H](O)C4)C)[C@@H](C(C=C5)=COC5=O)[C@@H](OC(C)=O)C[C@@]13O

For research use only. We do not sell to patients.


Summary

Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation [1] [2] .


In Vitro

Bufotalin (0.1-2.5 μM; 12-96 hours) treatment dose- and time-dependently inhibits MG-63 osteoblastoma cell survival [1] .
Bufotalin (0.5-2.5 μM; 48 hours) treatment dose-dependently increases the percentage of Annexin V positive cells (apoptotic cells) and caspase-12 activity in MG-63 cells. Bufotalin-induced osteoblastoma cell apoptosis is associated with caspase-12 activation [1] .
Bufotalin (0.5-2.5 μM; 12 hours) treatment dose-dependently induces C/EBP homologous protein (CHOP) expression as well as PERK and IRE1 phosphorylation in MG-63 cells. Bufotalin induces endoplasmic reticulum (ER) stress activation in cells [1] .
Bufotalin treatment induces cell cycle arrest at G2/M phase through down-regulation of Aurora A, CDC25, CDK1, cyclin A and cyclin B1, as well as up-regulation of p53 and p21 in HepG2 cells. Bufotalin treatment also induces apoptosis which was accompanied by decrease in mitochondrial membrane potential, increases in intracellular calcium level and reactive oxygen species production, activations of caspase-9 and -3, cleavage of poly ADP-ribose polymerase (PARP) as well as changes in the expressions of bcl-2 and bax [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay [1]

Cell Line: MG-63 osteoblastoma cells
Concentration: 0.1 μM, 0.5 μM, 1 μM, 2.5 μM
Incubation Time: 12 hours, 24 hours, 48 hours, 72 hours, 96 hours
Result: Inhibited MG-63 osteoblastoma cell survival.

Apoptosis Analysis [1]

Cell Line: MG-63 cells
Concentration: 0.5 μM, 1 μM, 2.5 μM
Incubation Time: 48 hours
Result: Dose-dependently increased the percentage of Annexin V positive cells (apoptotic cells) and caspase-12 activity in MG-63 cells.

Western Blot Analysis [1]

Cell Line: MG-63 cells
Concentration: 0.5 μM, 1 μM, 2.5 μM
Incubation Time: 12 hours
Result: Dose-dependently induced CHOP expression as well as PERK and IRE1 phosphorylation in MG-63 cells.

In Vivo

Bufotalin (0.5-1 mg/kg; intraperitoneal injection; twice daily; for 7 days) treatment shows a significantly reduced tumor growth in mice [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID male mice (4-6 weeks old) injected with U2OS cells [1]
Dosage: 0.5 mg/kg, 1 mg/kg
Administration: Intraperitoneal injection; twice daily; for 7 days
Result: Inhibited U2OS osteoblastoma cell growth in mice.

Appearance

Solid


Source

toad


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 4.6 mg/mL ( 10.35 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2494 mL 11.2471 mL 22.4942 mL
5 mM 0.4499 mL 2.2494 mL 4.4988 mL
10 mM 0.2249 mL 1.1247 mL 2.2494 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.62 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: 2.5 mg/mL (5.62 mM); Suspended solution; Need ultrasonic

* All of the co-solvents are available by MCE.


Synonyms

Bufa-20,22-dienolide, 16-(acetyloxy)-3,14-dihydroxy-, (3β,5β,16β)-
5β-Bufa-20,22-dienolide, 3β,14,16β-trihydroxy-, 16-acetate
(3β,5β,16β)-16-(Acetyloxy)-3,14-dihydroxybufa-20,22-dienolide
Bufotalin
3β,14,16β-Trihydroxy-5β-bufa-20,22-dienolide 16-acetate
NSC 89596