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SAR-020106

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].

Product Specifications

CAS Number

[1184843-57-9]

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

Available Sizes

Curated Selection

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