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NVP-TNKS656 98%

NVP-TNKS656

源葉(MedMol)
S80340
1419949-20-4
C27H34N4O5
494.5827
NVP-TNKS656, CAS#1419949-20-4, PARP抑制劑;TNKS-656; TNKS656; TNKS656(NVP-TNKS656); N-(cyclopropylmethyl)-2-(4-(4-methoxybenzoyl)piperidin-1-yl)-N-((4-oxo-4,5,7,8-tetrahydro-3H-pyrano[4,3-d]pyrimidin-2-yl
品牌 貨號(hào) 產(chǎn)品規(guī)格 價(jià)格(RMB) 庫(kù)存（上海） 北京 武漢 南京 購(gòu)買數(shù)量
源葉(MedMol) S80340-5mg 98% ￥770.00元 5 - - -
源葉(MedMol) S80340-10mg 98% ￥1270.00元 7 - - -
源葉(MedMol) S80340-25mg 98% ￥2700.00元 預(yù)計(jì)交期：2-3天 - - -
源葉(MedMol) S80340-100mg 98% ￥5700.00元 預(yù)計(jì)交期：2-3天 - - -
產(chǎn)品介紹 參考文獻(xiàn) 質(zhì)檢證書(shū)(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.
產(chǎn)品描述： NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.
靶點(diǎn)： TNKS2:6 nM (IC50);PARP2:32 μM (IC50);Apoptosis;PARP;Wnt/beta-catenin
體內(nèi)研究： NVP-TNKS656 (30 or 100 mg/kg, p.o.) exhibits good exposure and moderate oral bioavailability of 32% and 53%, respectively. Some slight overproportional increase in oral exposure is observed between 30 and 100 mg/kg with the dose normalized AUC for the 100 mg/kg dose being 2-fold higher than for the 30 mg/kg dose. Mice treated with NVP-TNKS656 (350 mg/kg, p.o.) show good plasma and tumor exposures corresponding to AUC0-24h of 515 and 325 μM·h, respectively.
參考文獻(xiàn)： 1: Shultz MD, Cheung AK, Kirby CA, Firestone B, Fan J, Chen CH, Chen Z, Chin DN, Dipietro L, Fazal A, Feng Y, Fortin PD, Gould T, Lagu B, Lei H, Lenoir F, Majumdar D, Ochala E, Palermo MG, Pham L, Pu M, Smith T, Stams T, Tomlinson RC, Tour? BB, Visser M, Wang RM, Waters NJ, Shao W. Identification of NVP-TNKS656: The Use of Structure-Efficiency Relationships To Generate a Highly Potent, Selective, and Orally Active Tankyrase Inhibitor. J Med Chem. 2013 Aug 22;56(16):6495-511. doi: 10.1021/jm400807n. Epub 2013 Aug 13. PubMed PMID: 23844574。
溶解性： soluble  in  DMSO
保存條件： -20℃
配置溶液濃度參考：
1mg 5mg 10mg
1 mM 2.022 ml 10.11 ml 20.219 ml
5 mM 0.404 ml 2.022 ml 4.044 ml
10 mM 0.202 ml 1.011 ml 2.022 ml
50 mM 0.04 ml 0.202 ml 0.404 ml
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參考文獻(xiàn)

質(zhì)檢證書(shū)(COA)

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