For research use only.

Catalog No.S7740

SAR-020106 Chemical Structure

CAS No. 1184843-57-9

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

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Biological Activity

Description SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM.
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. 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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-29 cells M2e4OWZ2dmO2aX;uJIF{e2G7 NF7oUldCdnSrbXn0c5Rq[yCjY4Tpeol1gSCrbjDleI9xd3OrZHWtbY5lfWOnZDDoeY1idiCKVD2yPUBk\WyuczDhd5Nme3OnZDDhd{BqdmS3Y4Tpc44hd2ZiTT3wbIF{\SCyaH;zdIhweHKxdHXpckAzKGW6cILld5Nqd25iYomgSWxKW0FuIFnDOVA:OC5yNUWg{txO M4HaZVIzOTFzOUK3
HEK cells MoHqSpVv[3Srb36gZZN{[Xl? NGfwR4NKdmirYnn0bY9vKG:oIHj1cYFvKEWURzDveoVz\XiycnXzd4VlKGmwIFjFT{Bk\WyuczygTWM2OD13IN88US=> M3TaVFI{ODh{OE[w
SW620 cells NG\lNIxHfW6ldHnvckBie3OjeR?= M2mwTWlvcGmkaYTpc44hd2ZiQ1jLNUBqdiCqdX3hckBUXzZ{MDDj[YxteyCjc4Pld5Nm\CCjczDwc5RmdnSrYYTpc44hd2ZiZ3XtZ4l1[WKrbnWtbY5lfWOnZDDjfZRwfG:6aXPpeJkh[W[2ZYKgNlQhfG9iNEigbJJ{ M1TzV|I{ODh{OE[w

... Click to View More Cell Line Experimental Data

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].


Cell Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: BALB/c mice
  • Dosages: 40 mg/kg
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 20 mg/mL (52.23 mM)
Ethanol 2 mg/mL (5.22 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 382.85


CAS No. 1184843-57-9
Storage powder
in solvent
Synonyms N/A
Smiles CC(CN(C)C)OC1=NC(=CN=C1C#N)NC2=NC=C3C(=C2)C=CC=C3Cl

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID