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| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


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| 描述 | Bufalin is an active component isolated from Chan Su, acts as a potent Na+/K+-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively[3]. Bufalin caused significant cytotoxicity in NCI-H460 cells at a concentration as low as 1 μM. DNA condensation was observed in bufalin-treated cells in a dose-dependent manner. Bufalin injected intraperitoneally in a dose-dependent manner reduced tumor size in BALB/C nu/nu mice implanted with NCI-H460 cells. Bufalin injection did not produce significant drug-related toxicity in experimental animals except at a high dose (0.4 mg/kg)[4]. Bufalin-induced disruption of the SRC-1 (steroid receptor coactivator) isoform/ERβ (estrogen receptor) axis might induce apoptosis, pyroptosis and ERS (endoplasmic reticulum-stress) signaling in endometriotic lesions, causing the suppression of endometriosis[5]. Bufalin inhibits cell proliferation and migration of HCC (hepatocellular carcinoma) cells via APOBEC3F induced intestinal immune network for IgA production signaling pathway[6]. |
| 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. |
| 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. |
| 计算器 | ||||
| 存储液制备 | ![]() |
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 |
|
| CAS号 | 465-21-4 |
| 分子式 | C24H34O4 |
| 分子量 | 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 |
| MDL No. | MFCD00056525 |
| 别名 | NSC 89595; BF |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C |
| 溶解方案 |
DMSO: 105 mg/mL(271.65 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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