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Chemical Structure| 1184843-57-9 Chemical Structure| 1184843-57-9

Structure of SAR-020106
CAS No.: 1184843-57-9

Chemical Structure| 1184843-57-9

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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.

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Product Details of SAR-020106

CAS No. :1184843-57-9
Formula : C19H19ClN6O
M.W : 382.85
SMILES Code : N#CC1=NC=C(NC2=CC3=C(C=N2)C(Cl)=CC=C3)N=C1O[C@H](C)CN(C)C
MDL No. :MFCD28155090

Safety of SAR-020106

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

Target
  • Chk1

    Chk1, IC50:13.3 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HO8910-DDP 1 µM 6 hours SAR-020106 weakened chemoresistance in cisplatin-resistant cells J Ovarian Res. 2021 Sep 3;14(1):115
A2780-DDP 1 µM 6 hours SAR-020106 weakened chemoresistance in cisplatin-resistant cells J Ovarian Res. 2021 Sep 3;14(1):115
P0306 0.25 µM 1 hour Evaluate the apoptosis-inducing effect of SAR on P0306 cells, results showed SAR significantly enhanced radiation-induced apoptosis J Exp Clin Cancer Res. 2019 Oct 21;38(1):420
P0297 0.25 µM 1 hour Evaluate the apoptosis-inducing effect of SAR on P0297 cells, results showed SAR significantly enhanced radiation-induced apoptosis J Exp Clin Cancer Res. 2019 Oct 21;38(1):420
DBTRG 0.25 µM 1 hour Evaluate the apoptosis-inducing effect of SAR on DBTRG cells, results showed SAR significantly enhanced radiation-induced apoptosis J Exp Clin Cancer Res. 2019 Oct 21;38(1):420
A172 0.25 µM 1 hour Evaluate the apoptosis-inducing effect of SAR on A172 cells, results showed SAR significantly enhanced radiation-induced apoptosis J Exp Clin Cancer Res. 2019 Oct 21;38(1):420
T98G 0.25 µM 1 hour Evaluate the apoptosis-inducing effect of SAR on T98G cells, results showed SAR significantly enhanced radiation-induced apoptosis J Exp Clin Cancer Res. 2019 Oct 21;38(1):420
LN405 0.25 µM 1 hour Evaluate the apoptosis-inducing effect of SAR on LN405 cells, results showed SAR significantly enhanced radiation-induced apoptosis J Exp Clin Cancer Res. 2019 Oct 21;38(1):420
DAOY cells 0.05–1 µM 72 hours SAR alone caused a concentration-dependent decrease in metabolic activity and proliferation, and when combined with RT, it enhanced these antitumor effects, including reduced proliferation, apoptosis, and clonogenicity, and increased residual DNA damage compared to RT alone. DAOY cells were slightly more sensitive than UW228 cells. Int J Mol Sci. 2025 Mar 13;26(6):2577
UW228 cells 0.05–1 µM 72 hours SAR alone caused a concentration-dependent decrease in metabolic activity and proliferation, and when combined with RT, it enhanced these antitumor effects, including reduced proliferation, apoptosis, and clonogenicity, and increased residual DNA damage compared to RT alone. Int J Mol Sci. 2025 Mar 13;26(6):2577

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice SW620 human colon carcinoma xenograft model Intraperitoneal injection 40 mg/kg Not used Evaluate the inhibitory effect of SAR-020106 on CHK1 and its combined therapeutic effect with irinotecan and gemcitabine J Med Chem. 2011 Dec 22;54(24):8328-42
NSG mice SHH/ p53-mut MB PDX model Intraperitoneal injection 40 mg/kg/d Once daily for 5 days SAR monotherapy initially enhanced tumor growth at d14 (3.32-fold), followed by growth inhibition compared to the control at d28–42. When combined with RT, high-dose SAR showed opposite effects, causing increased tumor mass. Int J Mol Sci. 2025 Mar 13;26(6):2577

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.06mL

2.61mL

1.31mL

26.12mL

5.22mL

2.61mL

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