SAR-020106

For research use only.

Catalog No.S7740

SAR-020106 Chemical Structure

Molecular Weight(MW): 382.85

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.
Targets
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 NIG4S2RHfW6ldHnvckBie3OjeR?= NFftSpNCdnSrbXn0c5Rq[yCjY4Tpeol1gSCrbjDleI9xd3OrZHWtbY5lfWOnZDDoeY1idiCKVD2yPUBk\WyuczDhd5Nme3OnZDDhd{BqdmS3Y4Tpc44hd2ZiTT3wbIF{\SCyaH;zdIhweHKxdHXpckAzKGW6cILld5Nqd25iYomgSWxKW0FuIFnDOVA:OC5yNUWg{txO MkT1NlIyOTF7Mke=
HEK cells MV;GeY5kfGmxbjDhd5NigQ>? NYfPNWc3UW6qaXLpeIlwdiCxZjDoeY1idiCHUlegc5ZmemW6cILld5Nm\CCrbjDISWsh[2WubIOsJGlEPTB;NTFOwG0> MmjSNlMxQDJ6NkC=
SW620 cells NHTxZ5hHfW6ldHnvckBie3OjeR?= M2jpUmlvcGmkaYTpc44hd2ZiQ1jLNUBqdiCqdX3hckBUXzZ{MDDj[YxteyCjc4Pld5Nm\CCjczDwc5RmdnSrYYTpc44hd2ZiZ3XtZ4l1[WKrbnWtbY5lfWOnZDDjfZRwfG:6aXPpeJkh[W[2ZYKgNlQhfG9iNEigbJJ{ MWKyN|A5Ojh4MB?=

... 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].

Protocol

Cell Research:[1]
- Collapse
  • 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
Formula

C19H19ClN6O

CAS No. 1184843-57-9
Storage powder
in solvent
Synonyms N/A
Smiles CC(CN(C)C)OC1=C(N=CC(=N1)NC2=NC=C3C(=CC=CC3=C2)Cl)C#N

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID