• 产品描述： SKLB-23bb is a potent and selective inhibitor for HDAC6 with an IC50 of 17 nM and shows 25-fold and 200-fold selectivity relative to HDAC1 (IC50=422 nM) and HDAC8 (IC50=3398 nM), respectively.

• 靶点： IC50: 17 nM (HDAC6), 422 nM (HDAC1), 398 nM (HDAC8);HDAC

• 体外研究：
  SKLB-23bb (Compound 23bb) presents low nanomolar antiproliferative effects against panel of cancer cell lines. The antiproliferative activity is ton human malignant melanoma A375 cells and cervical cancer HeLa cells, SKLB-23bb shows the most potent activities with IC50 values of 50 and 49 nM on A375 and HeLa cells, respectively. The antiproliferative activities against 11 kinds of hematological tumors (myelomaU266, RPMI8226 cells, human leukemia MV4-11, K562 cells, and human B cell lymphoma Ramos cells) or solid tumors (ovarian cancer A2780s, SKOV-3 cells, breast cancer SKBR3 cells, liver cancer HepG2 cells, lung cancer H460, A549 cells, cervical cancer HeLa cells and colon cancer HCT116, HT29 cells) cell lines of SKLB-23bb are evaluated by MTT, and the SAHA and ACY-1215 are as positive control. SKLB-23bb shows significant antiproliferative potential with the IC50 values ranging from 14 to 104 nM in these tumor cell lines

• 体内研究：
  SKLB-23bb (Compound 23bb) reduces the tumor growth in both the hematological tumor MV4-11 xenograft model and solid tumor HCT116 xenograft model. The significant antitumor activities are observed by intravenous administration of SKLB-23bb at 50 mg/kg on MV4-11 and HCT116 xenograft models. The growth of MV4-11 and HCT116 cancer cell xenografts is suppressed by 55.0% and 76.3% (percent of tumor mass change [TGI] values) after iv administration of SKLB-23bb at 50 mg/kg. The HCT116 xenograft model is also established to investigate the antitumor activity of oral administration of SKLB-23bb. The TGI value of oral administration of SKLB-23bb (25 mg/kg) on HCT116 xenograft model is 60.4%, which is superior to the SAHA group (100 mg/kg, 59.2%). Additionally, the body weight decrease is acceptable and no other adverse effects are observed upon treatment with SKLB-23bb. Low clearance (CL=7.008 L/kg per hour for iv, CL=12.877 L/kg per hour for po) and long terminal half-life (t1/2=7.658 h for iv, t1/2=9.62 h for po) are observed in SKLB-23bb. The oral bioavailability of SKLB-23bb is excellent in rats and the bioavailability is up to 47.0%

• 参考文献：
  1. Yang Z, et al. Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. J Med Chem. 2016 Feb 25;59(4):1455-70.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.522 ml	12.612 ml	25.224 ml
  5 mM	0.504 ml	2.522 ml	5.045 ml
  10 mM	0.252 ml	1.261 ml	2.522 ml
  50 mM	0.05 ml	0.252 ml	0.504 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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