bs-83013C

DATASHEET

Formulation Orange solid

Storage: -20°C

Product Information:

AZD7762 is a potent and selective inhibitor of checkpoint kinases 1 and 2 (IC50 = 5 nM for both).1 It abrogates DNA damage-induced S and G2 checkpoints and enhances the efficacy of DNA damaging agents such as gemcitabine and irinotecan. AZD7762 also enhanced the radiation sensitivity of p53-mutant tumor cell lines.2,3 AZD7762 was able to overcome imatinib resistance in CML cells.4 AZD7762 has also been reported to be a potent inhibitor of MEKK2 (MAP3K2) – IC50 = 20 nM.5 It has also recently been shown to inhibit antigen-stimulated degranulation from RBL-2H3 (IC50 = 28 nM) and BMMCs (IC50 = 99 nM) as well as suppressing degranulation of LAD2 human mast cells (IC50 = 50 nM) via Syk suppression through inactivation of Lyn and Fyn kinases.6

Description:

CAS Number: 860352-01-8 (free base) Chemical Name: 3-(Carbamoylamino)-5-(3-fluorophenyl)-N-[(3S)-piperidin-3-yl]thiophene-2-carboxamide Molecular weight: 398.88 Formula: C17H19FN4O2S·HCl Solubility: DMSO (>25 mg/ml) Physical Properties: Yellow/brown solid Purity: 98% by HPLC NMR (Conforms)