Veliparib dihydrochloride
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.
Veliparib dihydrochloride是一种有效的PARP1和PARP2抑制剂,K(i)值分别为5.2和2.9 nmol/L[1]。
PARP是聚ADP核糖聚合酶的简称,在多种癌症中过表达。由于多种癌症比起正常细胞更不依赖于PARP,使得PARP成为一种引人注目的癌症治疗目标。许多研究表明,PARP抑制剂在临床前研究的体外和体内模型中可作为放疗和化疗增敏剂[2][3]。
Veliparib dihydrochloride是一种PARP的选择性抑制剂。在结肠癌细胞系HCT-116和HT-29中,以veliparib dihydrochloride为佐剂与SN38或Oxall共同使用,可提高G2/M细胞周期停滞,并可通过抑制PARP-1和PARP-2提高DNA损伤水平[4]。
在皮下注射B16F10小鼠黑色素瘤细胞的小鼠模型中,口服剂量为3.1 mg/kg/d~25 mg/kg/d的veliparib dihydrochloride与temozolomide可提高药效,并显著减慢肿瘤发展。在MX-1乳腺癌异种移植模型(BRCA1缺失且BRCA2突变)或HCT-116结肠癌模型中也得到了相似的结果[1]。
参考文献:
[1]. Donawho, C.K., et al., ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models. Clin Cancer Res, 2007. 13(9): p. 2728-37.
[2]. Benafif, S. and M. Hall, An update on PARP inhibitors for the treatment of cancer. Onco Targets Ther, 2015. 8: p. 519-28.
[3]. Guillot, C., et al., PARP inhibition and the radiosensitizing effects of the PARP inhibitor ABT-888 in in vitro hepatocellular carcinoma models. BMC Cancer, 2014. 14: p. 603.
[4]. Davidson, D., et al., The PARP inhibitor ABT-888 synergizes irinotecan
treatment of colon cancer cell lines. Invest New Drugs, 2013. 31(2): p. 461-8.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 317.21 |
Cas No. | 912445-05-7 |
Formula | C13H18Cl2N4O |
Synonyms | ABT-888 dihydrochloride;ABT888 dihydrochloride;ABT 888 dihydrochloride |
Solubility | ≥31.7 mg/mL in DMSO; ≥104 mg/mL in H2O; ≥3.3 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide;dihydrochloride |
SDF | Download SDF |
Canonical SMILES | CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N.Cl.Cl |
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。 |
Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively. | ||||||
Targets | PARP1 | PARP2 | ||||
IC50 | 5.2 nM (Ki) | 2.9 nM (Ki) |
质量控制和MSDS
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