Home Cell Cycle Chk inhibitor SAR-020106 For research use only.

SAR-020106

SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM.

SAR-020106 Chemical Structure

SAR-020106 Chemical Structure

CAS: 1184843-57-9

Purity & Quality Control

Batch: S774001 DMSO] 20 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.01%
99.01

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-29 cells Function assay Antimitotic activity in etoposide-induced human HT-29 cells assessed as induction of M-phase phosphoprotein 2 expression by ELISA, IC50=0.055 μM 22111927
HEK cells Function assay Inhibition of human ERG overexpressed in HEK cells, IC50=5 μM 23082860
SW620 cells Function assay Inhibition of CHK1 in human SW620 cells assessed as potentiation of gemcitabine-induced cytotoxicity after 24 to 48 hrs 23082860
Click to View More Cell Line Experimental Data

Biological Activity

Description SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM.
Targets
Chk1 [1]
(Cell-free assay)
13.3 nM
In vitro
In vitro SAR-020106 abrogates an etoposide-induced G2 arrest with an IC50 of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion. SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion[1].
Cell Research Cell lines SW620 colon cancer cells
Concentrations 5 μM
Incubation Time 24 h
Method Cells were treated with SN38 (100 nmol/L) alone, with SAR-020106 alone (5 μmol/L), or with a fixed concentration of SN38 (100 nmol/L) in combination with increasing concentrations of SAR-020106 for 24 h.
In Vivo
In vivo SAR-020106 can enhance the antitumor effects of both irinotecan and gemcitabine in vivo with appropriate biomarker changes and minimal toxicity[1]. Although having minimal oral bioavailability in mice (F = 5%), distribution of SAR-020106 following i.p. dosing (40 mg/kg) was sufficient to inhibit CHK1 in the tumors, as shown by inhibition of the irinotecan-induced CHK1 pS296 autophosphorylation. At doses giving inhibition of CHK1 activity in vivo, the selective CHK1 inhibitor SAR-020106 showed no single agent activity in the SW620 xenograft model, and tumors grew at similar rates to the vehicle-treated controls. When dosed (i.p.) in combination with irinotecan, SAR-020106 was observed to potentiate the antitumor activity of the genotoxic drug in the SW620 xenograft model[2].
Animal Research Animal Models BALB/c mice
Dosages 40 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 382.85 Formula

C19H19ClN6O
CAS No. 1184843-57-9 SDF Download SAR-020106 SDF
Smiles CC(CN(C)C)OC1=NC(=CN=C1C#N)NC2=NC=C3C(=C2)C=CC=C3Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 20 mg/mL ( (52.23 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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