SAR-020106

SKU: orb1306399

Description

SAR-020106 is a selective, ATP-competitive small molecule inhibitor of CHK1, demonstrating potent activity with an IC50 of 13.3 nM. It is a valuable research tool for studying DNA damage response pathways and has been utilized in both in vitro and in vivo models of oncology research.

Research Area

Cell Biology

Key Properties

• CAS Number: 1184843-57-9
• MW: 382.85
• Purity: 95.11% (May vary between batches)
• Formula: C₁₉H₁₉ClN₆O
• SMILES: C[C@H](CN(C)C)Oc1nc(Nc2cc3cccc(Cl)c3cn2)cnc1C#N
• Target: Chk
• Solubility: DMSO:12 mg/mL (31.34 mM)

Bioactivity

• Target IC50:
  Chk1:13.3 nM (IC50)
• 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.
• In Vitro:
  SAR-020106 potentiated the efficacies of irinotecan and gemcitabine in SW620 human colon carcinoma xenografts in nude mice

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cycle, cells, colon, Checkpoint Kinase (Chk), CHK1, cancer, arrest, antitumor, inhibit, Inhibitor, selectivity, SAR 020106, SAR020106, SAR-020106, SN38, SW620

Compound Identifiers

PubChem CID

44203948