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Berzosertib (VE-822)

    99%

3-[3-[4-[(Methylamino)methyl]phenyl]-5-isoxazolyl]-5-[4-[(1-methylethyl)sulfonyl]phenyl]-2-pyrazinam

源葉(MedMol)
S80206
1232416-25-9
C24H25N5O3S
463.55
5-(4-(isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine; VE-822;
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) S80206-5mg 99% ¥340.00元 7 - - -
源葉(MedMol) S80206-10mg 99% ¥625.60元 7 - - -
源葉(MedMol) S80206-50mg 99% ¥1490.00元 4 - - -
產(chǎn)品介紹 參考文獻(xiàn) 質(zhì)檢證書(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

VE-822 has been used in trials studying the treatment of Ovarian Neoplasms, Ovarian Serous Tumor, Adult Solid Neoplasm, Advanced Solid Tumor, and Advanced Solid Neoplasm, among others.
產(chǎn)品描述: VE-822 has been used in trials studying the treatment of Ovarian Neoplasms, Ovarian Serous Tumor, Adult Solid Neoplasm, Advanced Solid Tumor, and Advanced Solid Neoplasm, among others.
靶點(diǎn): ATM/ATR
體內(nèi)研究: 80 nM VE-822單獨(dú)使用增加MiaPaCa-2和PSN-1細(xì)胞停留在G1期的比率。80 nM VE-822消除MiaPaCa-2和PSN-1細(xì)胞中富含XRT的G2/M期部分。VE-822單獨(dú)作用不大,而80 nM VE-822與XRT和/或gemcitabine聯(lián)用則增強(qiáng)PSN-1細(xì)胞中的早期和晚期細(xì)胞凋亡。VE-822增加對(duì)與pChk1 Ser345阻斷相關(guān)的DNA損傷劑的腫瘤應(yīng)答。VE-822(80 nM)減弱ATR信號(hào)傳導(dǎo)途徑并降低腫瘤細(xì)胞對(duì)XRT和吉西他濱的應(yīng)答的存活率。在正常細(xì)胞中,80 nM VE-822減弱ATR信號(hào)通路強(qiáng)度,但并沒有增強(qiáng)輻射和gemcitabine殺傷正常細(xì)胞的能力
細(xì)胞實(shí)驗(yàn): VE-822 is dissolved in DMSO and stored, and then diluted with appropriate media before use. Gemcitabine (10 nM) is added 24 h pre-XRT and is replaced with fresh medium before addition of VE-822. PSN-1 cells are treated with VE-822 (80 nM) for 1 h before, through to 18 h after, XRT (6 Gy). Apoptosis is analyzed 48 h after XRT by flow cytometry using an Annexin V-FITC kit with Pl
參考文獻(xiàn): 1.Fokas E, et al. Cancer Treat Rev, 2013, pii: S0305-7372(13)00065-0. 2.Fokas E, et al. Cell Death Dis, 2012, 3, e441. 3.Konstantinopoulos P A , Cheng S C , Hendrickson A E W , et al. Berzosertib plus gemcitabine versus gemcitabine alone in platinum-resistant high-grade serous ovarian cancer: a multicentre, open-label, randomised, phase 2 trial[J]. The Lancet Oncology, 2020, 21(7).
溶解性: DMSO:34  mg/mL  (73.3  mM)    Ethanol:<1  mg/mL
保存條件: 2-8℃
配置溶液濃度參考:
1mg 5mg 10mg
1 mM 2.157 ml 10.786 ml 21.573 ml
5 mM 0.431 ml 2.157 ml 4.315 ml
10 mM 0.216 ml 1.079 ml 2.157 ml
50 mM 0.043 ml 0.216 ml 0.431 ml
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參考文獻(xiàn)

質(zhì)檢證書(COA)

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摩爾濃度計(jì)算器

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