SAR-020106

• Description :

  SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents[1][2].

• UNSPSC :

  12352005

• Target :

  Checkpoint Kinase (Chk)

• Type :

  Reference compound

• Related Pathways :

  Cell Cycle/DNA Damage

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/sar-020106.html

• Concentration :

  10mM

• Purity :

  98.04

• Solubility :

  DMSO : 5 mg/mL (ultrasonic)

• Smiles :

  N#CC1=NC=C(NC2=CC3=C(C=N2)C(Cl)=CC=C3)N=C1O[C@H](C)CN(C)C

• Molecular Formula :

  C19H19ClN6O

• Molecular Weight :

  382.85

• References & Citations :

  [1]Walton MI, et al. The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106. Mol Cancer Ther. 2010;9 (1) :89-100.|[2]Reader JC, et al. Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. J Med Chem. 2011;54 (24) :8328-8342.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  Chk1

• CAS Number :

  [1184843-57-9]