AZD1152

• CAT Number: I004689
• CAS Number: 722543-31-9
• Molecular Formula: C26H31FN7O6P
• Molecular Weight: 587.5
• Purity: ≥95%
• Target: Aurora Kinase
• Solubility: DMSO: ≥ 33 mg/mL
• Storage: Store at -20°C
• IC50: 3-40 nM (HL-60, NB4, MOLM13; PALL-2; MV4-11; EOL-1; K562 cell) [1]
• IUPAC Name: 2-[ethyl-[3-[4-[[5-[2-(3-fluoroanilino)-2-oxoethyl]-1H-pyrazol-3-yl]amino]quinazolin-7-yl]oxypropyl]amino]ethyl dihydrogen phosphate
• InChI: InChI=1S/C26H31FN7O6P/c1-2-34(10-12-40-41(36,37)38)9-4-11-39-21-7-8-22-23(16-21)28-17-29-26(22)31-24-14-20(32-33-24)15-25(35)30-19-6-3-5-18(27)13-19/h3,5-8,13-14,16-17H,2,4,9-12,15H2,1H3,(H,30,35)(H2,36,37,38)(H2,28,29,31,32,33)
• InChIKey: GBJVVSCPOBPEIT-UHFFFAOYSA-N
• SMILES: CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCOP(=O)(O)O

AZD1152 (Cat.No:I004689) is a potent and selective inhibitor of Aurora kinase B, a key regulator of mitotic progression. It has demonstrated antitumor activity in preclinical models and is being investigated for the treatment of various cancers. AZD1152 has shown promising results in phase I and II clinical trials and is currently being evaluated in several ongoing clinical trials.

Reference

1:Barasertib (AZD1152), a Small Molecule Aurora B Inhibitor, Inhibits the Growth of SCLC Cell Lines In Vitro and In Vivo. Helfrich BA, Kim J, Gao D, Chan DC, Zhang Z, Tan AC, Bunn PA Jr.Mol Cancer Ther. 2016 Oct;15(10):2314-2322. Epub 2016 Aug 5. PMID: 27496133 2:[(14) C]-AZD1152 drug substance manufacture: challenges of an IV-infusion dosed human mass balance study in patients. Bushby N, Bergin J, Harding J.J Labelled Comp Radiopharm. 2016 May 30;59(6):250-4. doi: 10.1002/jlcr.3376. PMID: 27169761 3:Significance of AZD1152 as a potential treatment against Aurora B overexpression in acute promyelocytic leukemia. Ghanizadeh-Vesali S, Zekri A, Zaker F, Zaghal A, Yousefi M, Alimoghaddam K, Ghavamzadeh A, Ghaffari SH.Ann Hematol. 2016 Jun;95(7):1031-42. doi: 10.1007/s00277-016-2670-6. Epub 2016 Apr 19. PMID: 27091351 4:Inhibitor of Aurora Kinase B Induces Differentially Cell Death and Polyploidy via DNA Damage Response Pathways in Neurological Malignancy: Shedding New Light on the Challenge of Resistance to AZD1152-HQPA. Zekri A, Ghaffari SH, Yaghmaie M, Estiar MA, Alimoghaddam K, Modarressi MH, Ghavamzadeh A.Mol Neurobiol. 2016 Apr;53(3):1808-1823. doi: 10.1007/s12035-015-9139-9. Epub 2015 Mar 11. PMID: 25752998 5:A phase II trial of AZD1152 in relapsed/refractory diffuse large B-cell lymphoma. Collins GP, Eyre TA, Linton KM, Radford J, Vallance GD, Soilleux E, Hatton C.Br J Haematol. 2015 Sep;170(6):886-90. doi: 10.1111/bjh.13333. Epub 2015 Feb 26. No abstract available. PMID: 25721307 6:AZD1152-HQPA induces growth arrest and apoptosis in androgen-dependent prostate cancer cell line (LNCaP) via producing aneugenic micronuclei and polyploidy. Zekri A, Ghaffari SH, Ghanizadeh-Vesali S, Yaghmaie M, Salmaninejad A, Alimoghaddam K, Modarressi MH, Ghavamzadeh A.Tumour Biol. 2015 Feb;36(2):623-32. doi: 10.1007/s13277-014-2664-8. Epub 2014 Oct 3. PMID: 25277659 7:Phase I study assessing the safety and tolerability of barasertib (AZD1152) with low-dose cytosine arabinoside in elderly patients with AML. Kantarjian HM, Sekeres MA, Ribrag V, Rousselot P, Garcia-Manero G, Jabbour EJ, Owen K, Stockman PK, Oliver SD.Clin Lymphoma Myeloma Leuk. 2013 Oct;13(5):559-67. doi: 10.1016/j.clml.2013.03.019. Epub 2013 Jun 10. PMID: 23763917 Free PMC Article8:Stage I of a phase 2 study assessing the efficacy, safety, and tolerability of barasertib (AZD1152) versus low-dose cytosine arabinoside in elderly patients with acute myeloid leukemia. Kantarjian HM, Martinelli G, Jabbour EJ, Quintás-Cardama A, Ando K, Bay JO, Wei A, Gröpper S, Papayannidis C, Owen K, Pike L, Schmitt N, Stockman PK, Giagounidis A; SPARK-AML1 Investigators..Cancer. 2013 Jul 15;119(14):2611-9. doi: 10.1002/cncr.28113. Epub 2013 Apr 19. PMID: 23605952 Free PMC Article9:[Effect of aurora kinase B inhibitor AZD1152 in the treatment of cisplatin-resistant ovarian carcinoma]. Ma YX, Li XZ.Zhonghua Fu Chan Ke Za Zhi. 2013 Jan;48(1):46-50. Chinese. PMID: 23531251 10:Aurora kinase inhibitor AZD1152 has an additional effect of platinum on a sequential application at the human ovarian cancer cell line SKOV3. Ma Y, Weimer J, Fredrik R, Adam-Klages S, Sebens S, Caliebe A, Hilpert F, Eckmann-Scholz C, Arnold N, Schem C.Arch Gynecol Obstet. 2013 Jul;288(1):173-82. doi: 10.1007/s00404-013-2719-x. Epub 2013 Feb 7. PMID: 23389245