AZD7762 | Checkpoint kinase 1/2 inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $60.00 | ||
| 25 mg | $200.00 |
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 Enhances CRISPR-Cpf1-mediated precise genome editing.7
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
7) Ma et al. (2018) Small molecules promote CRISPR-Cpf1-mediated genome editing in human pluripotent stem cells; Nat. Commun. 9 1303
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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
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 Enhances CRISPR-Cpf1-mediated precise genome editing.7
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
7) Ma et al. (2018) Small molecules promote CRISPR-Cpf1-mediated genome editing in human pluripotent stem cells; Nat. Commun. 9 1303
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1-855-FOCUS21
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