my account
Login
  Loading... Please wait...

Product Details

AZD7762 | Checkpoint kinase 1/2 inhibitor

AZD7762 (860352-01-8, free base) 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

References/Citations
1) Zabludoff et al. (2008) AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies; Mol. Cancer Ther. 7 2955
2) Mitchell et al. (2010) In vitro and in vivo radiation sensitization of human tumor cells by a novel checkpoint kinase inhibitor, AZD7762; Clin. Cancer Res. 16 2076
3) Morgan et al. (2010) Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair; Cancer Res. 70 49721
4) Lei et al. (2018) Chk1 inhibitors overcome imatinib resistance in chronic myeloid leukemia cells; Leuk. Res. 64 17
5) Ahmad et al. (2015) Identification of Ponatinib and Other Known Kinase Inhibitors with Potent MEKK2 Inhibitory Activity; Biochem. Biophys. Res. Commun. 463 888
6) Park et al. (2018) Repositioning of anti-cancer drug candidate, AZD7762, to an anti-allergic drug suppressing IgE-mediated mast cells and allergic responses via the inhibition of Lyn and Fyn; Biochem. Pharmacol. 154 270

swipe
Image 1

Catalog#  10-4771-0005

$60.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
Request Bulk Quote
CAS:
860352-01-8 (free base)
Catalog Number:
10-4771
Activity:
Checkpoint kinase 1/2 inhibitor
Chemical Name:
3-(Carbamoylamino)-5-(3-fluorophenyl)-N-[(3S)-piperidin-3-yl]thiophene-2-carboxamide
Molecular Weight:
398.88
Molecular Formula:
C17H19FN4O2S • HCl
Solubility:
Soluble in DMSO (up to at least 25 mg/ml).
Physical Properties:
Yellow or brown solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

Connect with Focus

Click the button below to add the AZD7762 | Checkpoint kinase 1/2 inhibitor to your wish list.