R1530
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.
R1530是一种强效的和口服有效的有丝分裂/血管生成抑制剂[ 1 ]。
有丝分裂是细胞周期过程的一部分,通过有丝分裂,细胞核中的染色体分成位于各自细胞核中的两个相同的部分。血管生成涉及新生血管的生长,并且是肿瘤的发展和转移中必不可少的一部分[ 1 ]。
针对细胞周期蛋白依赖型激酶(例如CDK2和CDK4),以及血管生成相关的生长因子受体(例如KDR、FGFr、PDGFr以及EGFr),R1530显示强效的抑制作用[ 1 ]。在一系列人体肿瘤细胞系中,R1530抑制细胞生长,IC50值范围是0.22到3.43 μM。同时,R1530强力抑制由VEGF或bFGF驱动的人脐静脉内皮细胞(HUVEC)生长,IC50值分别为49 nM和118 nM [ 2 ]。
在带有人H460 肿瘤异种移植的裸鼠中,R1530 (3 到25 mg/kg,每天口服两次,20 天) 剂量依赖性地抑制肿瘤生长。R1530 (25 mg/kg剂量)平均减少肿瘤大小58%。
参考文献:
[1]. Liu JJ, Higgins B, Ju G, et al. Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors. ACS Med Chem Lett, 2013, 4(2): 259-263.
[2]. Kolinsky K, Tovar C, Zhang YE, et al. Preclinical evaluation of the novel multi-targeted agent R1530. Cancer Chemother Pharmacol, 2011, 68(6): 1585-1594.
[3]. Tovar C, Higgins B, Deo D, et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle, 2010, 9(16): 3364-3375.
Physical Appearance | Yellow solid |
Storage | Store at -20°C |
M.Wt | 356.78 |
Cas No. | 882531-87-5 |
Formula | C18H14ClFN4O |
Synonyms | R 1530;R-1530 |
Solubility | Soluble in DMSO |
Chemical Name | 5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydropyrazolo[3,4-b][1,4]benzodiazepine |
SDF | Download SDF |
Canonical SMILES | CC1=C2C(=NC3=CC(=C(C=C3C(=N2)C4=CC=CC=C4Cl)F)OC)NN1 |
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。 |