SAR-020106
| Code | Size | Price |
|---|
| SYN-1189-M100 | 100 mg | Enquire |
Quantity:
| SYN-1189-M050 | 50 mg | Enquire |
Quantity:
| SYN-1189-M001 | 1 mg | £233.00 |
Quantity:
| SYN-1189-M005 | 5 mg | £461.00 |
Quantity:
| SYN-1189-M010 | 10 mg | £719.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
4°C
Documents
Further Information
Alternate Names/Synonyms:
SAR020106
Appearance:
Solid.
CAS:
1184843-57-9
EClass:
32160000
Form (Short):
liquid
InChi:
InChI=1S/C19H19ClN6O/c1-12(11-26(2)3)27-19-16(8-21)22-10-18(25-19)24-17-7-13-5-4-6-15(20)14(13)9-23-17/h4-7,9-10,12H,11H2,1-3H3,(H,23,24,25)/t12-/m1/s1
InChiKey:
SRBJWIBAMIKCMV-GFCCVEGCSA-N
Long Description:
Chemical. CAS: 1184843-57-9. Formula: C19H19ClN6O. MW: 382.9. SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3nM on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55nM 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.
Molecular Formula:
C19H19ClN6O
Molecular Weight:
382.9
Package Type:
Plastic Vial
Product Description:
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3nM on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55nM 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.
Purity:
>95%
Solubility Chemicals:
Soluble in DMSO.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 1 year after receipt when stored at +4°C.
References
The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106: M.I. Walton, et al.; Mol. Cancer Ther. 9, 89 (2010) | The Chk1 inhibitor SAR-020106 sensitizes human glioblastoma cells to irradiation, to temozolomide, and to decitabine treatment: I. Patties, et al.; J. Exp. Clin. Cancer Res. 38, 420 (2019)