Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol/L on the isolated human enzyme.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 44.00 | |
5 mg | In stock | $ 97.00 | |
10 mg | In stock | $ 172.00 | |
25 mg | In stock | $ 347.00 | |
50 mg | In stock | $ 555.00 | |
100 mg | In stock | $ 783.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 116.00 |
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. |
Targets&IC50 | Chk1:13.3 nM (IC50) |
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]. |
Molecular Weight | 382.85 |
Formula | C19H19ClN6O |
CAS No. | 1184843-57-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12 mg/mL (31.34 mM)
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
SAR-020106 1184843-57-9 Cell Cycle/Checkpoint Chk SAR020106 cycle SN38 selectivity SW620 cancer inhibit colon cells SAR 020106 Checkpoint Kinase (Chk) antitumor arrest Inhibitor inhibitor