Molecular structure of AZD7762, CAS Number: 860352-01-8
AZD7762 (CAS 860352-01-8)
Alternate Names:
1-(2-((S)-piperidin-3-ylcarbamoyl)-5-(3-fluorophenyl)thiophen-3-yl)urea
Application:
AZD7762 is a checkpoint kinase inhibitor for Chk1 and Chk2
CAS Number:
860352-01-8
Purity:
≥98%
Molecular Weight:
362.42
Molecular Formula:
C17H19FN4O2S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
AZD7762 is a checkpoint kinase inhibitor for both Chk1 and Chk2. It is a more selective Chk1 inhibitor that competitively binds to the ATP-binding site of Chk1, reducing Chk1′s phosphorylation of a Cdc25C peptide. AZD7762 abrogates DNA damage-induced S and G2 checkpoints with an EC50 value of 10 nM and potentiates the efficacy of DNA-damage repair prohibitive agents, gemcitabine and topotecan, both in vitro and in various tumor xenografts by modulating downstream checkpoint pathway proteins.
AZD7762 (CAS 860352-01-8) References
- AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies. | Zabludoff, SD., et al. 2008. Mol Cancer Ther. 7: 2955-66. PMID: 18790776
- Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair. | Morgan, MA., et al. 2010. Cancer Res. 70: 4972-81. PMID: 20501833
- Potentiation of the novel topoisomerase I inhibitor indenoisoquinoline LMP-400 by the cell checkpoint and Chk1-Chk2 inhibitor AZD7762. | Aris, SM. and Pommier, Y. 2012. Cancer Res. 72: 979-89. PMID: 22189968
- The checkpoint kinase inhibitor AZD7762 potentiates chemotherapy-induced apoptosis of p53-mutated multiple myeloma cells. | Landau, HJ., et al. 2012. Mol Cancer Ther. 11: 1781-8. PMID: 22653969
- The Chk1 inhibitor AZD7762 sensitises p53 mutant breast cancer cells to radiation in vitro and in vivo. | Ma, Z., et al. 2012. Mol Med Rep. 6: 897-903. PMID: 22825736
- Checkpoint kinase inhibitor AZD7762 overcomes cisplatin resistance in clear cell carcinoma of the ovary. | Itamochi, H., et al. 2014. Int J Gynecol Cancer. 24: 61-9. PMID: 24362713
- Birinapant (TL32711) Improves Responses to GEM/AZD7762 Combination Therapy in Triple-negative Breast Cancer Cell Lines. | Min, DJ., et al. 2016. Anticancer Res. 36: 2649-57. PMID: 27272773
- Checkpoint kinase inhibitor AZD7762 strongly sensitises urothelial carcinoma cells to gemcitabine. | Isono, M., et al. 2017. J Exp Clin Cancer Res. 36: 1. PMID: 28049532
- 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. | Park, YH., et al. 2018. Biochem Pharmacol. 154: 270-277. PMID: 29777684
- Effects of a checkpoint kinase inhibitor, AZD7762, on tumor suppression and bone remodeling. | Wang, L., et al. 2018. Int J Oncol. 53: 1001-1012. PMID: 30015873
- Checkpoint kinase inhibitor AZD7762 enhance cisplatin-induced apoptosis in osteosarcoma cells. | Zhu, J., et al. 2019. Cancer Cell Int. 19: 195. PMID: 31372095
- Temozolomide and AZD7762 Induce Synergistic Cytotoxicity Effects on Human Glioma Cells. | Chen, Y., et al. 2020. Anticancer Res. 40: 5141-5149. PMID: 32878802
- Crystal Structure of the Kinase Domain of MerTK in Complex with AZD7762 Provides Clues for Structure-Based Drug Development. | Park, TH., et al. 2020. Int J Mol Sci. 21: PMID: 33114206
- Chk1/2 inhibitor AZD7762 enhances the susceptibility of IDH-mutant brain cancer cells to temozolomide. | Ozgiray, E., et al. 2022. Med Oncol. 39: 166. PMID: 35972603
- Chk1/2 inhibitor AZD7762 blocks the growth of preantral follicles by inducing apoptosis, suppressing proliferation, and interfering with the cell cycle in granulosa cells. | Liu, XM., et al. 2022. Histol Histopathol. 18547. PMID: 36398929
Inhibitor of:
ANKLE2, APC15, Ape2, APLF, ASCC1, BC066135, BC068157, Bcl-6b, BRAT1, C19orf39, C230055K05Rik, C3orf24, C6orf106_D17Wsu92e, CASC1, CCDC82, Cdc14a phosphatase, Cdc45, Cdt1, Chk1, Chk2, claudin-3, CWF19L2, CXorf57_D330045A20Rik, DBC1, EG546272, EG546282, ELOF1, ESCO2, EVI5L, F730047E07Rik, FAM136B, FAM175B, FAM35A, FMIP, fzr, GABP-α, Ggnbp2, HELB, IFN-α13, IL-10Rβ, IRF-2BP1, LOC342918, MDC1, MEI1, MIS12, MKS1, MOB3A, MYT1L, Ninein, NSE2, NSE4A, Olfr549, PNK, Rad17, Rad21, RAD51AP2, Rad55, Rad59, Rad9B, RFC1, RNF168, RNF23, RNF8, Rsk-2, Scc1, SERTAD3, SLD5, SMC1α, SMC6, STK31, TIM-1, TIPIN, TLK2, TNNI3K, TRF2, TSSK 1, TTBK1, TTBK2, TTI1, Vav, VPRBP, VRK2, VSIG (V-set and immunoglobulin domain containing), XRCC3, XRRA1, YY1AP1, ZIP-kinase, and ZNF26.Activator of:
APC5, BC055324, BC057079, BOB_GPR15, C10orf6, DNA Ligase III, DNA pol ε B, DUE-B, F730047E07Rik, FAM128B, FRMD6, Fyn, Histone H2A.X, ISG20, MASTL, MER3, Morc3, NDR1, Nek11, ORC5, Rad3, RCC2, RNase HII-A, Rnr1, SLX1A/B_SLX1, SSBP3, TopBP1, WAPL, and XLF.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
AZD7762, 2 mg | sc-364423 | 2 mg | $107.00 |