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抑制剂/激活剂

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凋亡与自噬

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Veliparib 维利帕尼; ABT-888

Veliparib (ABT-888) 是一种有效的 PARP 抑制剂，抑制 PARP1 和 PARP2 的 Ki 分别为 5.2 和 2.9 nM。

货号：
TK0232
规格：

1mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	912444-00-9
生物活性	Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.
分子式	C13H16N4O
分子量	244.29
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : ≥ 29 mg/mL (118.71 mM)
体内研究	Veliparib (ABT-888) is a potent inhibitor of PARP, has good oral bioavailability, can cross the blood-brain barrier in syngeneic and xenograft tumor models. In MDA-MB-231 xenograft tumor models, combination treatment (AG014699/PF-02341066 and Veliparib (ABT-888)/Foretinib) substantially reduced tumor growth compared to either inhibitor alone.
体外研究	Veliparib (ABT-888) is also tested against SIRT2, an enzyme that also uses NAD for catalysis, and found to be inactive (>5,000 nM). The receptor profile of Veliparib is determined in a panel of 74 receptor-binding assays at a concentration of 10 μM. Veliparib displaces control-specific binding at 50% or greater at the human H1(61%), the human 5-HT1A (91%), and the human 5-HT7 (84%) sites only. The IC50s for these three receptors are 5.3, 1.5, and 1.2 μM, respectively. c-Met knockdown cells show 4.2- (shMet-A; 95% CI=4-4.5) or 4.6-fold (shMet-B; 95% CI=4.4-4.8) growth inhibition when treated with 60 μM Veliparib (ABT-888). When treated with 38 μM Veliparib, c-Met knockdown cells show 2- (shMet-A; 95% CI=1.5-2.5) or 1.9-fold (shMet-B; 95% CI=1.3-2.5) growth inhibition. In HaCaT cells, at 6 h post-treatment by Veliparib (ABT-888), cell viability is significantly increases under 1,000 µM sulfur mustard (SM) exposure, whereas Veliparib does not protect cell viability under 100 µM SM exposure. Moreover, the addition of Veliparib no longer shows the protective effect at 24 h post SM exposure.
文献	•Cancer Discov. 2017 Sep;7(9):984-998. •Nat Commun. 2021 Jun 24;12(1):3931. •Theranostics. 2020 Jul 25;10(21):9477-9494. •Clin Cancer Res. 2017 Feb 15;23(4):1001-1011. •Cells. 2021, 10(3), 599. •Mol Cancer Ther. 2019 Nov;18(11):2063-2073. •Front Oncol. 2021 Jul 9;11:681441. •Acta Pharmacol Sin. 2021 Jul 22. •Neoplasia. 2019 Apr 24;21(6):533-544. •Neoplasia. 2018 Mar 28;20(5):478-488. •Front Mol Biosci. 2021 Apr 29;8:633344. •Nanomaterials. 2021, 11(6), 1514. •J Mol Med (Berl). 2019 Aug;97(8):1183-1193. •Cancer Genet. 2019 Nov;239:26-32. •J Chromatogr B Analyt Technol Biomed Life Sci. 2020 Oct 1;1154:122195. •J Vet Med Sci. 2018 Nov 23;80(11):1775-1781. •Research Square Preprint. 2021 Feb. •Patent. US20200129476A1 •Patent. US20200078369A1 •Patent. US20180362972A1. •Patent. US20180263995A1. •Int J Curr Res Acad Rev. 2017; 5(3): 53-64. •Electrostatics Joint Conference. 2016 July. •Harvard Medical School LINCS LIBRARY
纯度及产品资料	98%

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