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.
SAR-020106 细胞实验
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
SAR-020106 动物实验
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.
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