Bufalin (Synonyms: NSC 89595) |
カタログ番号GN10365
One-Click Copy Product Info
|
BufalinはNa+/K+-ATPase阻害剤である(α1: Kd = 42.5nM; α2: Kd = 45nM; α3: Kd = 40nM)。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 465-21-4
Sample solution is provided at 25 µL, 10mM.
BufalinはNa+/K+-ATPase阻害剤である(α1: Kd = 42.5nM; α2: Kd = 45nM; α3: Kd = 40nM)[1]。Bufalinは主に、細胞膜でNa⁺/K⁺-ATPaseの活性を阻害し、よって細胞内のカルシウム濃度を上昇させた[2]。Bufalinのアポトーシスの誘発と腫瘍細胞増殖の誘発は、オートファジーの惹起と腫瘍血管新生の阻害など、様々な抗腫瘍メカニズムを持つ[3]。Bufalinは、肝癌、肺癌、乳癌と白血病など様々な腫瘍の治療に使われる[4]。
NCI-H640細胞で、Bufalin (1μM, 2μM, 4μM; 24h)で処理した後、細胞の活性は著しく減少した[5]。Ishikawa, SK-OV-3とOMC-3卵巣癌細胞で、Bufalin (0.1-10ng/mL；48時間)は子宮内膜癌と卵巣癌細胞の増殖を阻害できる[6]。ヒトRCC ACHN細胞で、Bufalin (0-80nM；12-72時間)は、PI3K/Akt/mTORシグナル伝達経路を阻害することで、腎細胞癌の増殖と転移を抑制する[7]。
カラギーナン誘発性足浮腫ラットモデルで、Bufalin (0.15mg/kg, 0.3mg/kg, 0.6mg/kg；腹腔内；単回注射)の処理は、ラットの足浮腫の量を著しく減らした[8]。HCCLM3細胞転移性正所性腫瘍マウスモデルで、正所性移植腫瘍組織は、Bufalin (1mg/kg, 1.5mg/kg；腹腔内；30日間)の処理による壊死とアポトーシスを経験する[9]。
References:
[1]. Katz A, Lifshitz Y, Bab-Dinitz E, et al. Selectivity of digitalis glycosides for isoforms of human Na, K-ATPase[J]. Journal of Biological Chemistry, 2010, 285(25): 19582-19592.
[2]. Wu S H, Bau D T, Hsiao Y T, et al. Bufalin induces apoptosis in vitro and has Antitumor activity against human lung cancer xenografts in vivo[J]. Environmental Toxicology, 2017, 32(4): 1305-1317.
[3]. Yin P H, Liu X, Qiu Y Y, et al. Anti-tumor activity and apoptosis-regulation mechanisms of bufalin in various cancers: new hope for cancer patients[J]. Asian Pacific journal of cancer prevention, 2012, 13(11): 5339-5343.
[4]. Lan Y L, Lou J C, Jiang X W, et al. A research update on the anticancer effects of bufalin and its derivatives[J]. Oncology letters, 2019, 17(4): 3635-3640.
[5]. Wu S H, Wu T Y, Hsiao Y T, et al. Bufalin induces cell death in human lung cancer cells through disruption of DNA damage response pathways[J]. The American Journal of Chinese Medicine, 2014, 42(03): 729-742.
[6]. Takai N, Ueda T, Nishida M, et al. Bufalin induces growth inhibition, cell cycle arrest and apoptosis in human endometrial and ovarian cancer cells[J]. International journal of molecular medicine, 2008, 21(5): 637-643.
[7]. Xie J, Lin W, Huang L, et al. Bufalin suppresses the proliferation and metastasis of renal cell carcinoma by inhibiting the PI3K/Akt/mTOR signaling pathway[J]. Oncology letters, 2018, 16(3): 3867-3873.
[8]. Wen L, Huang Y, Xie X, et al. Anti‐inflammatory and antinociceptive activities of bufalin in rodents[J]. Mediators of inflammation, 2014, 2014(1): 171839.
[9]. Zhang Z J, Yang Y K, Wu W Z. Bufalin attenuates the stage and metastatic potential of hepatocellular carcinoma in nude mice[J]. Journal of translational medicine, 2014, 12(1): 57.
| 細胞実験[1]: | |
細胞株 | NCI-H640細胞 |
準備方法 | 12ウェルのプレートの中、約2 × 105細胞/ウェルのNCI-H640細胞を、0 (溶媒、0.5% DMSO), 1, 2と4μMの最終濃度のBufalinとともに24時間培養した。各処理からの細胞をPI (5 g/ml)で染色し、フローサイトメトリーで分析し、細胞の生存率を算出した。 |
反応条件 | 1μM, 2μM, 4μM；24時間 |
アプリケーション | Bufalinの処理後、細胞の活性は著しく減少した。 |
| 動物実験 [2]: | |
動物モデル | カラギーナン誘発性足浮腫ラットモデル |
準備方法 | 抗炎症作用は、カラギーナン誘発性足浮腫に基づいて評価した。Bufalin (0.15、0.3と0.6mg/kg、腹腔内注射)、indomethacin (10mg/kg、腹腔内注射)と溶媒を、カラギーナン注射の30分前に腹腔内注射した。各ラットの右後ろ足に、カラギーナン（生理食塩水に1% w/vで溶解した0.1mL）を足底注射した。カラギーナン注射の前、そしてその後の様々な時点（1、2、4と6時間）で、足浮腫の量を容積脈波計で測定した。カラギーナン注射前に測定した足の体積からの増加率で、足の腫脹率を算出した。最終評価の後、ラットの足を採取した。各後肢を踵骨のレベルで切断し、ウェスタンブロット解析に使用した。 |
投与形態 | 0.15mg/kg, 0.3mg/kg, 0.6mg/kg；腹腔内注射；単回注射 |
アプリケーション | Bufalin処理の後、ラットの足浮腫の量は著しく減少した。 |
References: | |
| Cas No. | 465-21-4 | SDF | |
| 同義語 | NSC 89595 | ||
| Chemical Name | 5-[(3S,5R,8R,9S,10S,13R,14S,17R)-3,14-dihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]pyran-2-one | ||
| Canonical SMILES | CC12CCC(CC1CCC3C2CCC4(C3(CCC4C5=COC(=O)C=C5)O)C)O | ||
| Formula | C24H34O4 | M.Wt | 386.52 |
| 溶解度 | ≥ 38.7mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5872 mL | 12.9359 mL | 25.8719 mL |
| 5 mM | 517.4 μL | 2.5872 mL | 5.1744 mL |
| 10 mM | 258.7 μL | 1.2936 mL | 2.5872 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)