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• 產(chǎn)品描述： Zabadinostat (CXD101) is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. Zabadinostat has no activity against HDAC class II. Zabadinostat has antitumor activity

• 靶點(diǎn)： HDAC1:63 nM (IC50);HDAC3:550 nM (IC50);HDAC2:570 nM (IC50);HDAC

• 體外研究：
  Zabadinostat has been tested in vitro in colon, lung, non-Hodgkin lymphoma, and myeloma cell lines with IC50s ranged from 0.2 to 15 μM

• 體內(nèi)研究：
  Zabadinostat substantially reduces tumor size in murine xenograft lung (A549a) and colon (HT29) models at a dose of 50 mg/kg. Tumor reductions are found to be associated with increased histone acetylation and decreased HDAC enzyme activity. For Zabadinostat, after oral dosing in murine and canine models, peak plasma concentrations (Cmax) are reached 1 to 2 hours after the dose and terminal half‐lives are 6 hours and 8 hours, respectively. After murine oral [14C]-Zabadinostat at a dose of 1.6 mg/kg (4 μmol/kg), tissue radioactivity peaked 3 to 6 hours after the dose and declined slowly thereafter with Zabadinostat‐related material still present in tissue 21 days after the dose

• 參考文獻(xiàn)：
  1. Eyre TA, et al. Predictive biomarkers for disease sensitivity in lymphoma - the holy grail for HDAC inhibitors? Oncotarget. 2018 Dec 18;9(99):37280-37281. 2. Eyre TA, et al. A phase 1 study to assess the safety, tolerability, and pharmacokinetics of CXD101 in patients with advanced cancer. Cancer. 2019 Jan 1;125(1):99-108.

• 溶解性： Soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.478 ml	12.391 ml	24.782 ml
  5 mM	0.496 ml	2.478 ml	4.956 ml
  10 mM	0.248 ml	1.239 ml	2.478 ml
  50 mM	0.05 ml	0.248 ml	0.496 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *