Telocinobufagin
Based on 1 publication(s) in Google Scholar
Telocinobufagin (Telobufotoxin; Telocinobufogenin) is an orally active bufadienolide with potential anti-tumor effects. Telocinobufagin exerts its anti-cancer effects on non-small cell carcinoma, osteosarcoma, thyroid cancer, breast cancer and head and neck squamous cell carcinoma by inhibiting the STAT3, JAK2/STAT3, LARP1-mTOR, PI3K/Akt/Snail and PLK1 pathways, and can also induce tumor cell apoptosis. Telocinobufagin enhances the Th1 immune response and protects against Salmonella typhimurium infection. Telocinobufagin has a strong cardiac-stimulating effect by inhibiting the activity of Na+/K+-ATPase, and it can promote renal fibrosis. Telocinobufagin demonstrates non-opioid analgesic effects in various acute pain models.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.50%
- CAS 番号: 472-26-4
- 分子式: C24H34O5
- 分子量:402.52
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 Telocinobufagin
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生物活性
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STAT3 |
JAK2 |
PLK1 |
Akt |
PI3K |
mTOR |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.1244 μM
Compound: Tel
|
Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 35200033] |
| A549 | IC50 |
3 μM
Compound: 10
|
Cytotoxicity against human A549 cells after 24 hrs by MTT assay
Cytotoxicity against human A549 cells after 24 hrs by MTT assay
|
[PMID: 24050254] |
| HepG2 | IC50 |
2.4 μM
Compound: 10
|
Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay
|
[PMID: 24050254] |
| HL-60 | IC50 |
<0.01 μg/mL
Compound: 19
|
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
|
[PMID: 11575946] |
| KB | IC50 |
1.3 μg/mL
Compound: 19
|
Cytotoxicity against human KB cells after 72 hrs by MTT assay
Cytotoxicity against human KB cells after 72 hrs by MTT assay
|
[PMID: 11575946] |
| MH60 | IC50 |
>25 μg/mL
Compound: 19
|
Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay
Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay
|
[PMID: 11575946] |
| NCI-H1299 | IC50 |
0.1066 μM
Compound: Tel
|
Cytotoxicity in human NCI-H1299 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity in human NCI-H1299 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 35200033] |
| PC-9 | IC50 |
0.6185 μM
Compound: Tel
|
Cytotoxicity in human PC-9 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity in human PC-9 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 35200033] |
| SK-MEL | IC50 |
0.05 μM
Compound: 8
|
Cytotoxicity against human SK-MEL cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Cytotoxicity against human SK-MEL cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
|
[PMID: 33882233] |
Telocinobufagin (0.01-100 μM, 0-96 h) suppresses proliferation and metastasis in human NSCLC cells, osteosarcoma cells, anaplastic thyroid cancer (ATC) cells, 4T1 breast cancer cells and neck squamous cell carcinoma (HNSCC)[1][2][6][7][8][9].
Telocinobufagin (0.125-5 μM, 24-48 h) induces apoptosis in human NSCLC cells and osteosarcoma cells and HNSCC cells[1][2][9].
Telocinobufagin (1-5 μM) induces G2/M phase arrest in Cal-27 cells and SCC-25 cells[9].
Telocinobufagin (0.5 μg/mL) suppresses malignant metastasis of undifferentiated thyroid carcinoma via modulation of the LARP1-mTOR pathway in CAL-62 cells[6].
Telocinobufagin (0.1-1 μM, 2-48 h) blocks STAT3 and JAK2/STAT3 signaling and inhibits PLK1[1][2][9].
Telocinobufagin (0.05-0.5 μg/mL, 24 h) reverses the epithelial-mesenchymal transition (EMT) process in breast cancer cells, downregulates the Snail transcription factor, and inhibits the PI3K/Akt/ERK signaling pathway.
Telocinobufagin (10-100 nM, 24 h) activates the pro-fibrotic phenotype of renal tubular epithelial cells (HK2 cells) and primary normal human renal mesangial cells (NHMCs), but is ineffective against SYF fibroblasts[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, PC9, and H1299 cells
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Concentration:0.01, 0.1, 1, 10, 100 μM
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Incubation Time:48 h
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Result:Inhibited cell viability in a concentration-dependent manner, and the corresponding half-maximal inhibitory concentrations (IC50) were 124.4, 618.5, and 106.6 nM, respectively.
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Cell Line:A549, PC9, and H1299 cells
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Concentration:0.125, 0.25 and 0.5 μM
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Incubation Time:PC9 and H1299 cells for 8 h, and A549 cells for 24 h
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Result:Remarkably suppressed cell migration in the Transwell migration assay.
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Cell Line:PC9, and H1299 cells
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Concentration:0.125, 0.25 and 0.5 μM
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Incubation Time:24 h (H1299) or 48 h (PC9)
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Result:Increased the apoptotic rates in both cell lines in a concentration-dependent manner.
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Cell Line:A549, PC9, and H1299 cells
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Concentration:0.25, 0.5 and 1 μM
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Incubation Time:4, 6, 8, 12 h
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Result:Strongly upregulated cleaved PARP1 protein, but down-regulated anti-apoptotic BCL2 protein.
Inhibited STAT3 phosphorylation at tyrosine 705 (Y705) and its downstream targets.
Inhibited STAT3 nuclear translocation in a concentration-dependent manner.
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Cell Line:143B, HOS, MG63, U2OS, SJSA and Saos-2 cells
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Concentration:0, 0.05, 0.1, 0.2, 0.5 and 1 μM
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Incubation Time:48 h
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Result:Inhibited cell proliferation in six osteosarcoma cell lines in a concentration-dependent manner.
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Cell Line:143B and HOS cells
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Concentration:0.1, 0.2 and 0.5 μM
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Incubation Time:12 h
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Result:Displayed strong inhibitory activity against tumor cell migration.
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Cell Line:143B and HOS cells
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Concentration:0.1, 0.2 and 0.5 μM
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Incubation Time:12 h
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Result:Displayed strong inhibitory activity against tumor cell invasion.
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Cell Line:143B and HOS cells
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Concentration:0.2 and 0.5 μM
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Incubation Time:48 h
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Result:Significantly induced tumor cell apoptosis.
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Cell Line:143B, HOS and MG63 cells
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Concentration:0.1, 0.2 and 0.5 μM
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Incubation Time:2, 4, 8, 12, 24, 48 h
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Result:Exhibited a dose-dependent significant inhibition of STAT3 phosphorylation and STAT3 phosphorylation induced by IL-6.
Down-regulated Cyclin D1, Bcl-2, Mcl-1 and Survivin.
Selectively inhibited the phosphorylation of JAK2, and had no significant effect on JAK1 and JAK3.
Down-regulated Snail and vimentin, and up-regulated E-cadherin.
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Cell Line:HK2 cells, NHMCs, SYF, SYF + cSrc cells
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Concentration:10 and 100 nM
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Incubation Time:24 h
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Result:Caused a dose-dependent increase in the expression of collagen 1 and collagen 3 mRNA in HK2 cells.
Significantly increased the expression of collagen 1 in NHMCs.
Increased collagen 1, collagen 3, TGFβ, CTGF mRNA.
Did not cause significant changes in the above indicators in the SYF cells.
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Cell Line:4T1 cells
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Concentration:0.05 and 0.5 μg/mL
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Incubation Time:24 h
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Result:Concentration-dependently inhibited 4T1 cell migration and significantly reduced the number of cells passed through.
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Cell Line:4T1 cells
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Concentration:0.05 and 0.5 μg/mL
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Incubation Time:24 h
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Result:Effectively inhibited the movement of cells through the matrix gel.
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Cell Line:4T1 cells
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Concentration:0.05 and 0.5 μg/mL
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Incubation Time:24 h
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Result:Increased the expression of the epithelial marker E-cadherin and reduced the expression of interstitial markers vimentin and fibronectin.
Significantly reduced the level of Snail protein and had no significant effect on other EMT transcription factors (Slug, Twist1, Zeb1, Zeb2).
Reduced the protein levels of p-Akt, p-mTOR and p-ERK and did not affect the expression of total Akt, mTOR and ERK proteins.
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Cell Line:Cal-27 and SCC-25 cells
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Concentration:1, 2, 4, 6, 8, 16, 32, 64, 128, 256, 512, 1024 μM
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Incubation Time:24 h
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Result:Exhibited IC50s against Cal-27 and SCC-25 cells of 7.97 and 5.39 μM.
Telocinobufagin (5-10 mg/kg, i.p., every 2 days for 20 days) significantly suppresses tumor growth and metastasis by inhibiting the JAK2/STAT3 signaling pathway in an osteosarcoma xenograft model in mice[2].
Telocinobufagin (10-40 μg, s.c., two doses, 14-day interval) enhances a Th1 immune response to control intracellular S. typhimurium infections in mice[3].
Telocinobufagin (0.062-10 mg/kg, i.p. and p.o, single dose) exhibits potent analgesic effects in various acute pain models in mice, and it does not rely on the opioid system or affect motor function. Its analgesic potency is four times that of morphine[4].
Telocinobufagin (0.1 mg/kg, i.p., once daily for 4 weeks) promotes renal fibrosis via Na+/K+-ATPase profibrotic signaling pathways[5].
Telocinobufagin (10-20 µg/mouse, i.p., 3 times a day for 2 weeks) inhibits breast cancer tumor growth and the epithelial mesenchymal transition in 4T1 cells xenograft model in mice[7][8].
Telocinobufagin (4-16 mg/kg, i.p., once daily for 30 days) inhibits tumor growth and lung metastasis in HNSCC cells-bearing mice[9].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A549 xenograft tumor model established in female nude mice (BALB/c nude, 4-5-week-old)[1]
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Dosage:1 and 2 mg/kg
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Administration:Intraperitoneal injection (i.p.), every 2 days for a total of 18 days
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Result:Significantly reduced tumor size. Showed no weight loss and had no noticeable toxicity on the heart, liver, lungs, or kidneys at this concentration. Reduced the expression of PSTAT3Y705, MCL1, and BCL2 and increased the levels of cleaved PARP1.
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Animal Model:143B cells xenograft tumor model established in male nude mice (BALB/c nude, 6-8-week-old)[2]
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Dosage:5 mg/kg and 10 mg/kg
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Administration:Intraperitoneal injection (i.p.), every 2 days for a total of 20 days
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Result:Significantly reduced tumor weights. Reduced the numbers of metastatic nodules.
Reduced the levels of phospho-STAT3 and phospho-JAK2.
Increased the proportion of cleaved caspase-3-positive tumor cells.
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Animal Model:S. typhimurium infection model established in female ICR mice (five weeks old, Grade II)[3]
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Dosage:10, 20, and 40 μg dissolved in saline
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Administration:Subcutaneous injection (s.c.), two doses on day 1 and day 15
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Result:Increased the survival rate of mice and reduced bacterial load.
Increased the levels of specific IgG2a (Th1-related antibodies) in OVA and FIST, while the level of IgG1 (Th2-related antibody) did not change significantly.
Promoted the secretion of IFN-γ (a key cytokine for Th1 cells) by spleen cells, but inhibited IL-4 (a marker for Th2 cells) and IL-17A (a marker for Th17 cells).
Upregulated the mRNA expression of the transcription factor T-bet (a key regulatory factor for Th1 cells), while having no significant effect on GATA-3 (Th2) and RORγt (Th17).
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Animal Model:Acetic acid-induced writhing test, formalin test, tail-flick test, hot-plate test, open-field test, rotarod test established in male Swiss Webster mice (25-30 g)[4]
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Dosage:0.062, 0.125, 0.25, 0.5, and 1 mg/kg (i.p.) and 0.625, 1.125, 2.5, 5, and 10mg/kg (p.o.)
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Administration:Intraperitoneal injection (i.p.) and oral administration (p.o.), single dose
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Result:Significantly inhibited the number of contortions in mice in a dose-dependent manner.
Significantly inhibited the licking time during the first 5 minutes after intraplantar injection of formalin.
Significantly increased the reaction time (the withdrawal by a brief vigorous movement) in a dose-dependent manner.
Significantly increased the reaction time (the withdrawal by a brief vigorous movement) in a dose-dependent manner.
Presented significant reaction latencies for 3 hours after administration (1 mg/kg, i.p; 10 mg/kg, p.o).
Did not affect locomotion in mice in open-field test and rotarod test.
Exhibited the potency about 4 times higher than that of morphine.
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Animal Model:Measurement of renal fibrosis model established in wild-type male SvJ/Black Swiss mice (25-30 g) (WT), as well as SvJ/Black Swiss mice heterozygous for the Na+/K+-ATPase-α-1 (referred to as NKA α-1+/−)[5]
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Dosage:0.1 mg/kg
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Administration:Intraperitoneal injection (i.p.), once daily for 4 weeks
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Result:Caused a significant increase in systolic blood pressure in both wild-type mice and NKAα-1+/− mice, but at 4 weeks, the amount of urinary protein excreted by NKAα-1+/− mice was significantly less than that of the wild-type control group.
Resulted in mild to moderate periglomerular and peritubular fibrosis of the renal cortex and the degree of renal fibrosis in NKAα-1+/− mice was lower than that in the wild-type control group at 4 weeks.
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Animal Model:
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Dosage:10 or 20 µg/mouse
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Administration:Intraperitoneal injection (i.p.), three times a week for two consecutive weeks.
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Result:Significantly reduced the tumor volume and weight.
Reduced the number of lung metastatic lesions
Observed EMT markers and signaling pathway proteins in tumor tissues consistent with those in the in vitro experiments.
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Animal Model:Cal-27 cells xenograft tumor model and normal or PLK1 over-expressed HNSCC cells induced lung metastasis model established in BALB/c nude mice[9]
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Dosage:4, 8, and 16 mg/kg (xenograft tumor model) and 8 mg/kg (lung metastasis model)
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Administration:Intraperitoneal injection (i.p.), once daily for 30 days
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Result:Significantly inhibited the growth of transplanted tumors and lung metastasis.
Downregulated the expressions of PLK1, CDC25c and Ki67 in tumor tissues and overexpression of PLK1 can completely reverse the anti-tumor effect of TBG.
化学情報
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CAS 番号 472-26-4
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性状 Solid
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分子量 402.52
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分子式 C24H34O5
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Color White to off-white
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SMILES
O[C@@]([C@@]1(CC2)C)(CC[C@@H]1C(C=C3)=COC3=O)[C@@](CC[C@@]45O)([H])[C@@]2([H])[C@]4(CC[C@H](O)C5)C
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別名
Telobufotoxin; Telocinobufogenin
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Structure Classification
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Initial Source
toad
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
-
Most Recent
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Phytomedicine
Telocinobufagin, a PLK1 suppressor that inhibits tumor growth and metastasis by modulating CDC25c and CTCF in HNSCC cells. [Abstract]2024 May:127:155440. PMID: 38452691
溶剤 & 溶解度
DMSO : 50 mg/mL (124.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.21 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (307 KB)
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- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Shen Y, et al. Telocinobufagin Has Antitumor Effects in Non-Small-Cell Lung Cancer by Inhibiting STAT3 Signaling. J Nat Prod. 2022 Apr 22;85(4):765-775. [Content Brief]
[2]. Ma X, et al. Telocinobufagin inhibits osteosarcoma growth and metastasis by inhibiting the JAK2/STAT3 signaling pathway. Eur J Pharmacol. 2023 Mar 5;942:175529. [Content Brief]
[3]. Wu SC, et al. Telocinobufagin enhances the Th1 immune response and protects against Salmonella typhimurium infection. Int Immunopharmacol. 2015 Apr;25(2):353-62. [Content Brief]
[4]. Feitosa GIMC,et al. Potent nonopioid antinociceptive activity of telocinobufagin in models of acute pain in mice. Pain Rep. 2019 Oct 8;4(6):e791. [Content Brief]
[5]. Kennedy DJ, et al. Telocinobufagin, a Novel Cardiotonic Steroid, Promotes Renal Fibrosis via Na⁺/K⁺-ATPase Profibrotic Signaling Pathways. Int J Mol Sci. 2018 Aug 29;19(9):2566. [Content Brief]
[6]. Qiang LZ, Fang SZ. Telocinobufagin suppresses malignant metastasis of undifferentiated thyroid carcinoma via modulation of the LARP1-mTOR pathway. Kaohsiung J Med Sci. 2025 Mar;41(3):e12934. [Content Brief]
[7]. Gao Y, et al. Telocinobufagin inhibits the epithelial-mesenchymal transition of breast cancer cells through the phosphoinositide 3-kinase/protein kinase B/extracellular signal-regulated kinase/Snail signaling pathway. Oncol Lett. 2018 May;15(5):7837-7845. [Content Brief]
[8]. Gao Y, et al. Erratum: Telocinobufagin inhibits the epithelial-to-mesenchymal transition of breast cancer cells through the PI3K/Akt/Snail signaling pathway. Oncol Lett. 2021 Apr;21(4):242. doi: 10.3892/ol.2021.12503. Epub 2021 Jan 31. Erratum for: Oncol Lett. 2018 May;15(5):7837-7845. [Content Brief]
[9]. Li J, et al. Telocinobufagin, a PLK1 suppressor that inhibits tumor growth and metastasis by modulating CDC25c and CTCF in HNSCC cells. Phytomedicine. 2024 May;127:155440. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4843 mL | 12.4217 mL | 24.8435 mL | 62.1087 mL |
| 5 mM | 0.4969 mL | 2.4843 mL | 4.9687 mL | 12.4217 mL | |
| 10 mM | 0.2484 mL | 1.2422 mL | 2.4843 mL | 6.2109 mL | |
| 15 mM | 0.1656 mL | 0.8281 mL | 1.6562 mL | 4.1406 mL | |
| 20 mM | 0.1242 mL | 0.6211 mL | 1.2422 mL | 3.1054 mL | |
| 25 mM | 0.0994 mL | 0.4969 mL | 0.9937 mL | 2.4843 mL | |
| 30 mM | 0.0828 mL | 0.4141 mL | 0.8281 mL | 2.0703 mL | |
| 40 mM | 0.0621 mL | 0.3105 mL | 0.6211 mL | 1.5527 mL | |
| 50 mM | 0.0497 mL | 0.2484 mL | 0.4969 mL | 1.2422 mL | |
| 60 mM | 0.0414 mL | 0.2070 mL | 0.4141 mL | 1.0351 mL | |
| 80 mM | 0.0311 mL | 0.1553 mL | 0.3105 mL | 0.7764 mL | |
| 100 mM | 0.0248 mL | 0.1242 mL | 0.2484 mL | 0.6211 mL |