Ro3280
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.
Ro3280是PLK1的选择性抑制剂,其IC50值为3 nM[1]。
Polo样激酶1(PLK1)是一种酶,在调控细胞周期中起着重要作用,早期触发G2向M期过渡。实验表明,PLK1在多种癌细胞中过表达,因而有望作为抗癌药物的靶点[2]。
在多种急性白血病细胞系中,Ro3280抑制U937、HL-60、NB4、K562、MV4-11和CCRF,相应IC50值分别为186 nM、175 nM、74 nM、797 nM、120 nM和162 nM。值得注意的是,与AML细胞(IC50值范围为52.80 ~ 147.50 nM)相比,ALL细胞(IC50值范围为35.49 ~ 110.76 nM)对Ro3280更为敏感。此外,Ro3280治疗降低细胞活力、诱导细胞凋亡以及扰乱细胞周期[3]。在H82(肺癌)、HT-29(结肠癌)、MDA-MB-468(乳腺癌)、PC3(前列腺癌)和A375(皮肤癌)中,Ro3280治疗抑制PLK1,相应IC50值为5 nM、10 nM、19 nM、12 nM和70 nM[1]。
在HT-29细胞皮下异种移植裸鼠模型中,给予40 mg/kg的Ro3280,一周一次,可以显著消退78%的肿瘤,而在更高的药物剂量以及给药频率下,Ro3280可以完全消退肿瘤[1]。
参考文献:
[1]. Chen, S., et al., Identification of novel, potent and selective inhibitors of Polo-like kinase 1. Bioorg Med Chem Lett, 2012. 22(2): p. 1247-50.
[2]. Czaplinski, S., et al., Polo-like kinase 1 inhibition sensitizes neuroblastoma cells for vinca alkaloid-induced apoptosis. Oncotarget, 2015.
[3]. Wang, N.N., et al., Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells. Int J Mol Sci, 2015. 16(1): p. 1266-92.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 543.61 |
Cas No. | 1062243-51-9 |
Formula | C27H35F2N7O3 |
Solubility | ≥27.2 mg/mL in DMSO; insoluble in H2O; ≥24.75 mg/mL in EtOH |
Chemical Name | 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-8H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide |
SDF | Download SDF |
Canonical SMILES | CN1CCC(CC1)NC(=O)C2=CC(=C(C=C2)NC3=NC=C4C(=N3)N(CC(C(=O)N4C)(F)F)C5CCCC5)OC |
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。 |
Description | Ro3280是一种有效的Polo样激酶1(PLK1)高选择性抑制剂,其IC50值为3 nM。 | |||||
靶点 | PLK1 | |||||
IC50 | 3?nM |
质量控制和MSDS
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