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• 产品描述： CHIR-124 is a potent and selective Chk1 inhibitor with IC50 of 0.3 nM, and also potently targets PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM.

• 靶点： Chk1:0.3 nM (IC50);Chk2:697.4 nM (IC50);PDGFR:6.6 nM (IC50);FLT3:5.8 nM (IC50);Cdk4/cyclin D:2.05 μM (IC50);CDC2/cyclin B:0.5057 μM (IC50);Cdk2/cyclin A:0.1911 μM (IC50);bFGFR:2.01 μM (IC50);FGFR3:1.29 μM (IC50);VEGFR2 FLK1:0.5779 μM (IC50);VEGFR1 FLT1:0.4636 μM (IC50);PKCα:0.58 μM (IC50);PKAβ I:2.25 μM (IC50);PKCβ II:0.58 μM (IC50);PKCγ:0.11 μM (IC50);ERK2:4.31 μM (IC50);PKA:0.1031 μM (IC50);GSK3:0.0233 μM (IC50);Apoptosis;GSK-3;FLT;Chk;PDGFR;Src

• 体内研究：
  CHIR-124 (10 or 20 mg/kg, p.o.) does not have a significant effect on tumor growth when compared with the vehicle-treated group, but it potentiates the growth inhibitory effect of CPT-11 in a human breast carcinoma xenograft model. The potentiation of the tumor growth inhibitory effect of CPT-11 by CHIR-124 is associated with an increase in apoptosis induction in the tumors. CHIR-124 reverses the suppression of phospho-H3 staining induced by CPT-11, indicating abrogation of the G2-M checkpoint by CHIR-124

• 参考文献：
  1. Tse AN, et al. CHIR-124, a novel potent inhibitor of Chk1, potentiates the cytotoxicity of topoisomerase I poisons in vitro and in vivo. Clin Cancer Res, 2007, 13(2 Pt 1), 591-602. 2. Dai Y, et al. New insights into checkpoint kinase 1 in the DNA damage response signaling network. Clin Cancer Res, 2010, 16(2), 376-383.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.381 ml	11.907 ml	23.815 ml
  5 mM	0.476 ml	2.381 ml	4.763 ml
  10 mM	0.238 ml	1.191 ml	2.381 ml
  50 mM	0.048 ml	0.238 ml	0.476 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 *