SAR-020106, inhibitor
SAR-020106
Purity
97.78%
Synonyms
SAR-020106; SAR020106; inhibitor
Purity/Purification
97.78%
Form/Format
Solid. Powder
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
Formula
C19H19ClN6O
SMILES
C[C@H](CN(C)C)Oc1nc(Nc2cc3cccc(Cl)c3cn2)cnc1C#N
CAS Number
1184843-57-9
In Vitro
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3nMol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55nMol/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 deathours. 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].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Related Product Information for SAR-020106, inhibitor
SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3nMol/L on the isolated human enzyme.
Product Categories/Family for SAR-020106, inhibitor
References
Walton M I, Eve P D, Hayes A, et al. The Preclinical Pharmacology and Therapeutic Activity of the Novel CHK1 Inhibitor SAR-020106[J]. Molecular Cancer Therapeutics, 2010, 9(1):89-100.
Klair S, Matthews T P, Cheung K M J, et al. Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing[J]. Journal of Medicinal Chemistry, 2011, 54(24):8328-42.
Klair S, Matthews T P, Cheung K M J, et al. Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing[J]. Journal of Medicinal Chemistry, 2011, 54(24):8328-42.
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Product Notes
The SAR-020106 (Catalog #AAA5756703) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "SAR-020106, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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