Home Cell Cycle Chk inhibitor SAR-020106

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SAR-020106 Chk inhibitor

Cat.No.S7740

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

Chemical Structure

Molecular Weight: 382.85

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

Cell Culture, Treatment & Working Concentration

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
HEK cells Function assay Inhibition of human ERG overexpressed in HEK cells, IC50=5 μM
SW620 cells Function assay Inhibition of CHK1 in human SW620 cells assessed as potentiation of gemcitabine-induced cytotoxicity after 24 to 48 hrs
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 382.85 Formula

C19H19ClN6O

 Storage (From the date of receipt)
CAS No. 1184843-57-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(CN(C)C)OC1=NC(=CN=C1C#N)NC2=NC=C3C(=C2)C=CC=C3Cl

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
Chk1 [1]
(Cell-free assay)
13.3 nM
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. This compound inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion[1].
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 this compound 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, this compound 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, this compound was observed to potentiate the antitumor activity of the genotoxic drug in the SW620 xenograft model[2].
References

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