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• 产品描述： SCH900776 (S-isomer) is an effective, specific and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50: 3 nM). It also inhibitors Chk2 (IC50: 1500 nM) and cyclin-dependent kinase CDK2 (IC50: 160 nM)

• 靶点： Chk;CDK

• 体外研究：
  SCH 900776 does not significantly inhibit HLMs CYP450 isoforms 1A2, 2C9, 2C19, 2D6, and 3A4. SCH 900776 induces a dose-dependent loss of DNA replication capability 24 hours after hydroxyurea exposure. In combination with an antimetabolite, SCH 900776 induces accumulation of γ-H2AX within 2 hours, indicative of replication fork collapse and double-stranded DNA breaks. SCH 900776 also dose-dependently suppresses accumulation of the Chk1 pS296 autophosphorylation.

• 体内研究：
  After pretreatment 30 minutes with gemcitabine, SCH 900776 (4 mg/kg) is sufficient to induce the γ-H2AX biomarker while 8 mg/kg leads to enhanced tumor pharmacodynamic and regression responses relative to gemcitabine or SCH 900776 alone. SCH 900776 (16/32 mg/kg) dose-dependently induces improvements in tumor response. Doses of SCH 900776 associate with robust biomarker activation and improved tumor response are not associated with enhanced toxicity of gemcitabine on hematological parameters in BALB/c mice.

• 参考文献：
  1. Montano R, et al. Preclinical development of the novel Chk1 inhibitor SCH900776 in combination with DNA-damaging agents and antimetabolites. Mol Y Ther. 2012 Feb;11(2):427-38. 2. Guzi TJ, et al. Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening. Mol Y Ther, 2011, 10(4), 591-602. 3. Thompson R, et al. The Mre11 nuclease is critical for the sensitivity of cells to Chk1 inhibition. PLoS One. 2012;7(8):e44021.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.658 ml	13.289 ml	26.578 ml
  5 mM	0.532 ml	2.658 ml	5.316 ml
  10 mM	0.266 ml	1.329 ml	2.658 ml
  50 mM	0.053 ml	0.266 ml	0.532 ml

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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 *