BI6727 (Volasertib)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BI6727(Volasertib)是一种选择性的Plk抑制剂,作用于Plk1、Plk2和Plk3,IC50值分别为0.87、5和56 nM[1]。
Polo-like kinase 1 (Plk1) 触发G2 / M期过渡,在许多癌症中过表达,被认识是癌症治疗的有效靶点[1]。
BI6727(Volasertib)是一种有效的Plk1的抑制剂,被认为是临床上很有前途的抗癌药。在NB TICs和正常人儿科SKPs(神经嵴样干细胞)中,BI6727(Volasertib)抑制NB TICs和SKPs,EC50值分别为21 nM和2.8 μM,减少TIC存活[2]。据报道,BI6727 (Volasertib)抑制多个肿瘤细胞系的增殖,包括HCT 116(结肠癌)、NCI-H460(肺癌)、BRO(黑色素瘤)和GRANTA(血癌),EC50值分别为23 nM、21 nM、11 nM和15 n[1] [3]。
在HCT 16细胞皮下异种移植裸鼠模型中,BI6727 (Volasertib) 口服给药后增加有丝分裂指数和细胞凋亡,从而延缓肿瘤生长,减少肿瘤大小,并诱导肿瘤消退。同样的结果在NCI-H4660(非小细胞肺癌)异种移植模型中也有出现[1]。
参考文献:
[1]. Rudolph, D., et al., BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity. Clin Cancer Res, 2009. 15(9): p. 3094-102.
[2]. Grinshtein, N., et al., Small molecule kinase inhibitor screen identifies polo-like kinase 1 as a target for neuroblastoma tumor-initiating cells. Cancer Res, 2011. 71(4): p. 1385-95.
[3]. Munch, C., et al., Therapeutic polo-like kinase 1 inhibition results in mitotic arrest and subsequent cell death of blasts in the bone marrow of AML patients and has similar effects in non-neoplastic cell lines. Leuk Res, 2015. 39(4): p. 462-70.
2. Zheng DW, Xue YQ, et al. "Volasertib suppresses the growth of human hepatocellular carcinoma in vitro and in vivo." Am J Cancer Res. 2016 Nov 1;6(11):2476-2488. PMID:27904765
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 618.83 |
Cas No. | 755038-65-4 |
Formula | C34H50N8O3 |
Synonyms | BI 6727; BI-6727 |
Solubility | insoluble in H2O; ≥10.31 mg/mL in DMSO; ≥56.1 mg/mL in EtOH |
Chemical Name | N-[4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexyl]-4-[[(7R)-7-ethyl-5-methyl-6-oxo-8-propan-2-yl-7H-pteridin-2-yl]amino]-3-methoxybenzamide |
SDF | Download SDF |
Canonical SMILES | CCC1C(=O)N(C2=CN=C(N=C2N1C(C)C)NC3=C(C=C(C=C3)C(=O)NC4CCC(CC4)N5CCN(CC5)CC6CC6)OC)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
人黑色素瘤A375和 Hs 294T细胞 |
溶解方法 |
在DMSO中的溶解度大于10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
24 h,10-100 nM |
应用 |
BI6727 (Volasertib) 是一个二代的Plk1小分子抑制剂,有研究报道它是有前景的治疗多种癌症的药物。BI6727 (Volasertib)可以抑制黑色素瘤细胞的生长和活力,并且诱导细胞凋亡。 |
临床实验[2]: | |
疾病模型 |
大于18周岁的患有局部晚期或转移的尿路上皮癌症病人 |
剂量 |
2小时静脉注射300 mg,每3周治疗周期的第一天给药 |
应用 |
对于晚期或转移的尿路上皮癌症病人,BI6727 (Volasertib)具有可接受的安全性,但是作为单一疗法抗肿瘤活性较小。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1]. Cholewa B D, Ndiaye M A, Huang W, et al. Small molecule inhibition of polo-like kinase 1 by volasertib (BI 6727) causes significant melanoma growth delay and regression in vivo[J]. Cancer Letters, 2017, 385: 179-187. [2]. Stadler W M, Vaughn D J, Sonpavde G, et al. An open‐label, single‐arm, phase 2 trial of the polo‐like kinase inhibitor volasertib (BI 6727) in patients with locally advanced or metastatic urothelial cancer[J]. Cancer, 2014, 120(7): 976-982. |
描述 | BI6727是一种高效的Polo-like kinase(Plk)抑制剂,IC50值为0.87 nM。 | |||||
靶点 | Polo-like kinase | |||||
IC50 | 0.87 nM |
质量控制和MSDS
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