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ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors SAR-020106

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SAR-020106 NEW

$44.00 1mg

$97.00 5mg

$172.00 10mg

Min. Order
Purity97.78%
Cas No1184843-57-9
Supply Ability10g
Update time2026-04-14

TargetMol Chemicals Inc.

TargetMol Chemicals Inc.

VIP6Y

United States

United States

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Chemical Properties

Product Name	SAR-020106
CAS No	1184843-57-9
EC-No
Min. Order
Purity	97.78%
Supply Ability	10g
Release date	2026/04/14

Product Introduction

Bioactivity

Name	SAR-020106
Description	SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol/L on the isolated human enzyme.
In vitro	SAR-020106 potentiated the efficacies of irinotecan and gemcitabine in SW620 human colon carcinoma xenografts in nude mice[2]
In vivo	SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) 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. Biomarker studies have shown that SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion both in vitro and in vivo. Cytotoxic drug combinations were associated with increased gammaH2AX and poly ADP ribose polymerase cleavage consistent with the SAR-020106-enhanced DNA damage and tumor cell death. Irinotecan and gemcitabine antitumor activity was enhanced by SAR-020106 in vivo with minimal toxicity. SAR-020106 represents a novel class of CHK1 inhibitors that can enhance antitumor activity with selected anticancer drugs in vivo and may therefore have clinical utility[1].
Storage	Shipping with blue ice/Shipping at ambient temperature.
Solubility Information	DMSO : 12 mg/mL (31.34 mM), Sonication is recommended.
Keywords	SW620 \| SN38 \| selectivity \| SAR-020106 \| SAR020106 \| SAR 020106 \| Inhibitor \| inhibit \| cycle \| colon \| CHK1 \| Checkpoint Kinase (Chk) \| cells \| cancer \| arrest \| antitumor
Inhibitors Related	Rabusertib \| CCT245737 \| Tuvusertib \| Prexasertib \| PD0166285 \| CHK1-IN-3 \| CHK1-IN-4 hydrochloride \| Protein kinase inhibitor 6 \| Prexasertib dihydrochloride \| ANI-7 \| BX795 \| M2I-1
Related Compound Libraries	Bioactive Compound Library \| Kinase Inhibitor Library \| Post-Translational Modification Compound Library \| Inhibitor Library \| NO PAINS Compound Library \| Bioactive Compounds Library Max \| Covalent Inhibitor Library \| Cell Cycle Compound Library \| Anti-Cancer Compound Library \| Anti-Cancer Active Compound Library

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