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ABT-888 (Veliparib)PARP抑制剂

ABT-888 (Veliparib)

产品编号:A3002
规格 单价 库存 订购数量
10mM (in 1mL DMSO) ¥638.00 现货
5mg ¥610.00 现货
10mg ¥890.00 现货
50mg ¥2,190.00 现货
200mg ¥6,270.00 现货

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Sample solution is provided at 25 µL, 10mM.

引用文献

1. Wang X, Sekine Y, et al. "Inhibition of Poly-ADP-Ribosylation Fails to Increase Axonal Regeneration or Improve Functional Recovery after Adult Mammalian CNS Injury." eNeuro. 2016 Dec 26;3(6). PMID:28032120
2. Nassour J, Martien S, et al."Defective DNA single-strand break repair is responsible for senescence and neoplastic escape of epithelial cells." Nat Commun. 2016 Jan 29;7:10399. PMID:26822533
3. Yalon M, Tuval-Kochen L, et al. "Overcoming Resistance of Cancer Cells to PARP-1 Inhibitors with Three Different Drug Combinations." PLoS One. 2016 May 19;11(5):e0155711. PMID:27196668

质量控制

化学结构

ABT-888 (Veliparib)

相关生物数据

ABT-888
ABT-888 enhances the antitumor activity of temozolomide in the rat 9L glioma orthotopic model. Tumor cells were inoculated into rat brain as described in Materials and Methods. The vehicle for the temozolomide and ABT-888 was saline. ABT-888 was administered at 25 mg/kg/dose, bd, orally, on days 2 to 17. Starting on day 4, temozolomide was administered at 17.5 mg/kg, qd, orally, on day 4 to 8 at 2 h post the morning dose of ABT-888.

相关生物数据

ABT-888

相关生物数据

ABT-888

ABT-888 (Veliparib) Dilution Calculator

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化学性质

CAS号 912444-00-9 SDF Download SDF
别名 ABT-888,ABT 888,ABT888,Veliparib
化学名 1-[3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one
SMILES CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N
分子式 C13H16N4O 分子量 244.3
溶解性 >6.1mg/mL in DMSO 储存条件 Store at -20°C
运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

生物活性

Veliparib (ABT-888)是一个有效的PARP1和PARP2抑制剂,Ki值分别为5.2 nM和2.9 nM。.
靶点 PARP1 PARP2        
IC50 5.2 nM (Ki) 2.9 nM (Ki)        

实验操作

细胞实验:

细胞系

HCT-116和HT-29细胞系

溶解方法

在DMSO中的溶解度>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

4 μM;24 h

应用

在HCT-116和HT-29细胞系中,用SRB实验检测ABT-888对抗癌剂SN38或oxaliplatin的协同作用。在SN38与ABT-888联合处理的样品中,PARP的活性显著减少(>4倍;24 h)。

动物实验:

动物模型

雌性无胸腺裸鼠

剂量

12.5 mg/kg;口服给药,2次/天,间隔6小时。

应用

在5-6周龄的雌性无胸腺裸鼠中,在每侧的皮下注射200 mL细胞悬浮液(5*106细胞)建立HCT116异种移植物。与RT和CPT-11,而非ABT-888治疗的肿瘤相比,三重疗法组(RT、CPT-11和ABT)具有显著更长的肿瘤生长延迟(TGD),其平均TGD为14.21天。

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] Davidson D, Wang Y, Aloyz R, et al. The PARP inhibitor ABT-888 synergizes irinotecan treatment of colon cancer cell lines[J]. Investigational new drugs, 2013, 31(2): 461-468.

[2] Shelton J W, Waxweiler T V, Landry J, et al. In vitro and in vivo enhancement of chemoradiation using the oral parp inhibitor ABT-888 in colorectal cancer cells[J]. International Journal of Radiation Oncology* Biology* Physics, 2013, 86(3): 469-476.

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研究更新

2. The PARP inhibitor ABT-888 synergizes irinotecan treatment of colon cancer cell lines. Invest New Drugs. 2013 Apr;31(2):461-8. doi: 10.1007/s10637-012-9886-7. Epub 2012 Oct 9.
Abstract
Treatments of ABT-888 (0.125 μΜ) with irinotecan and ABT-888 (0.5-4 μM) both exhibited synergistic effect against colon cancer cell lines, in which the synergy of ABT-888/irinotecan is correlated with the degree of PARP1 inhibition and results in increased G2/M cell cycle arrest and increased DNA damage after 24 h and increased apoptosis after 48 h.
4. Enhancement of synthetic lethality via combinations of ABT-888, a PARP inhibitor, and carboplatin in vitro and in vivo using BRCA1 and BRCA2 isogenic models. Mol Cancer Ther. 2012 Sep;11(9):1948-58. doi: 10.1158/1535-7163.MCT-11-0597. Epub 2012 Jul 9.
Abstract
ABT-888/carboplatin treatment exhibits a stronger ability to kill or inhibit proliferation of Brca/BRCA-deficient cells than cisplatin or carboplatin alone, which delayed tumor growth in Brca2 xenografts and induced DNA damage and apoptosis.
5. Phase I study of PARP inhibitor ABT-888 in combination with topotecan in adults with refractory solid tumors and lymphomas. Cancer Res. 2011 Sep 1;71(17):5626-34. doi: 10.1158/0008-5472.CAN-11-1227. Epub 2011 Jul 27.
Abstract
The combination of ABT-888 (10 mg) and topotecan (0.6 mg/m2/d) was orally administered to enrolled patients twice a day for the first 5 days during a 21-day cycle, in which a >75% reduction in PAR levels, a >50% reduction in PBMCs and increased γH2AX response in CTC and PBMCs were observed in patients.

产品描述

ABT-888 (Veliparib)是聚(ADP-核糖)聚合酶(PARP)的抑制剂。在临床前肿瘤模型中,ABT-888 (Veliparib)与各种细胞毒性药物联合使用显示了良好的体内功效。PARP参与DNA修复。PARP水平的升高会导致对细胞毒性化疗和放疗的抵抗性。因此,PARP抑制剂有望用于化疗和放疗的增敏剂。与微卫星稳定(MSS)的细胞系相比,ABT-888在MRE11和RAD50基因突变的微卫星不稳定性(MSI)细胞系中也是有活性的。

参考文献:
1. Shivaani Kummar, Robert Kinders, Martin E. Gutierrez, Larry Rubinstein, Ralph E. Parchment, Lawrence R. Phillips, Jiuping Ji, Anne Monks, Jennifer A. Low, Alice Chen, Anthony J. Murgo, Jerry Collins, Seth M. Steinberg, Helen Eliopoulos, Vincent L. Giranda, Gary Gordon, Lee Helman, Robert Wiltrout, Joseph E. Tomaszewski and James H. Doroshow. Phase 0 Clinical Trial of the Poly (ADP-Ribose) Polymerase Inhibitor ABT-888 in Patients With Advanced Malignancies. Journal of Clinical Oncology. 2009; 27(16): 2705 – 11.
2.  Xiaofeng Li, Juergen Delzer, Richard Voorman, Sonia M. de Morais and Yanbin Lao. Disposition and Drug-Drug Interaction Potential of Veliparib (ABT-888), a Novel and Potent Inhibitor of Poly (ADP-ribose) Polymerase. DRUG METABOLISM AND DISPOSITION. 2011; 39(7): 1161 – 69.
3.  E. Vilar Sanchez, A. Chow, L. Raskin, M. D. Iniesta, B. Mukherjee and S. B. Gruber. Preclinical testing of the PARP inhibitor ABT-888 in microsatellite instable colorectal cancer. Journal of Clinical Oncology. 2009; 27(15S): 11028A.