For research use only, not for therapeutic use.
SB-715992（Cat No.:I003220）is a potent, selective inhibitor of the protein kinase CK2, known for its role in cellular proliferation and survival. This compound has shown promise in preclinical studies for its potential to suppress tumor growth and enhance apoptosis in various cancer types. By disrupting CK2 activity, SB-715992 may offer a novel therapeutic approach in oncology, particularly for tumors resistant to conventional therapies. Ongoing research aims to elucidate its mechanism of action and explore its efficacy in combination with other anticancer agents, highlighting its potential in targeted cancer treatment strategies.
| Catalog Number | I003220 |
| CAS Number | 336113-53-2 |
| Synonyms | N-(3-aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxoquinazolin-2-yl)-2-methylpropyl]-4-methylbenzamide |
| Molecular Formula | C₃₀H₃₃ClN₄O₂ |
| Purity | ≥95% |
| Target | Ksp |
| Solubility | DMSO 100 mg/mL Ethanol 100 mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 1.7 nM(Ki) |
| IUPAC Name | N-(3-aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxoquinazolin-2-yl)-2-methylpropyl]-4-methylbenzamide |
| InChI | InChI=1S/C30H33ClN4O2/c1-20(2)27(34(17-7-16-32)29(36)23-12-10-21(3)11-13-23)28-33-26-18-24(31)14-15-25(26)30(37)35(28)19-22-8-5-4-6-9-22/h4-6,8-15,18,20,27H,7,16-17,19,32H2,1-3H3/t27-/m1/s1 |
| InChIKey | QJZRFPJCWMNVAV-HHHXNRCGSA-N |
| SMILES | CC1=CC=C(C=C1)C(=O)N(CCCN)[C@@H](C2=NC3=C(C=CC(=C3)Cl)C(=O)N2CC4=CC=CC=C4)C(C)C |
| Reference | </br>1:/Snapshots/ of ispinesib-induced conformational changes in the mitotic kinesin Eg5. Kaan HY, Major J, Tkocz K, Kozielski F, Rosenfeld SS.J Biol Chem. 2013 Jun 21;288(25):18588-98. doi: 10.1074/jbc.M113.462648. Epub 2013 May 8. PMID: 23658017 Free PMC Article</br>2:The structure of the ternary Eg5-ADP-ispinesib complex. Talapatra SK, Schüttelkopf AW, Kozielski F.Acta Crystallogr D Biol Crystallogr. 2012 Oct;68(Pt 10):1311-9. Epub 2012 Sep 13. PMID: 22993085 Free PMC Article</br>3:Phase I dose-escalation and pharmacokinetic study of ispinesib, a kinesin spindle protein inhibitor, administered on days 1 and 15 of a 28-day schedule in patients with no prior treatment for advanced breast cancer. Gomez HL, Philco M, Pimentel P, Kiyan M, Monsalvo ML, Conlan MG, Saikali KG, Chen MM, Seroogy JJ, Wolff AA, Escandon RD.Anticancer Drugs. 2012 Mar;23(3):335-41. doi: 10.1097/CAD.0b013e32834e74d6. PMID: 22123335 </br>4:A pediatric phase I trial and pharmacokinetic study of ispinesib: a Children/’s Oncology Group phase I consortium study. Souid AK, Dubowy RL, Ingle AM, Conlan MG, Sun J, Blaney SM, Adamson PC.Pediatr Blood Cancer. 2010 Dec 15;55(7):1323-8. doi: 10.1002/pbc.22609. Epub 2010 Aug 13. PMID: 20712019 Free PMC Article</br>5:A phase I study of ispinesib, a kinesin spindle protein inhibitor, administered weekly for three consecutive weeks of a 28-day cycle in patients with solid tumors. Burris HA 3rd, Jones SF, Williams DD, Kathman SJ, Hodge JP, Pandite L, Ho PT, Boerner SA, Lorusso P.Invest New Drugs. 2011 Jun;29(3):467-72. doi: 10.1007/s10637-009-9374-x. Epub 2010 Jan 13. PMID: 20069338 </br>6:Activity of the kinesin spindle protein inhibitor ispinesib (SB-715992) in models of breast cancer. Purcell JW, Davis J, Reddy M, Martin S, Samayoa K, Vo H, Thomsen K, Bean P, Kuo WL, Ziyad S, Billig J, Feiler HS, Gray JW, Wood KW, Cases S.Clin Cancer Res. 2010 Jan 15;16(2):566-76. doi: 10.1158/1078-0432.CCR-09-1498. Epub 2010 Jan 12. PMID: 20068098 Free PMC Article</br>7:Thermodynamics of nucleotide and inhibitor binding to wild-type and ispinesib-resistant forms of human kinesin spindle protein. Sheth PR, Basso A, Duca JS, Lesburg CA, Ogas P, Gray K, Nale L, Mannarino AF, Prongay AJ, Le HV.Biochemistry. 2009 Nov 24;48(46):11045-55. doi: 10.1021/bi900946r. PMID: 19824700 </br>8:Initial testing (stage 1) of the kinesin spindle protein inhibitor ispinesib by the pediatric preclinical testing program. Carol H, Lock R, Houghton PJ, Morton CL, Kolb EA, Gorlick R, Reynolds CP, Maris JM, Keir ST, Billups CA, Smith MA.Pediatr Blood Cancer. 2009 Dec 15;53(7):1255-63. doi: 10.1002/pbc.22056. PMID: 19554570 Free PMC Article</br>9:Southwest Oncology Group phase II study of ispinesib in androgen-independent prostate cancer previously treated with taxanes. Beer TM, Goldman B, Synold TW, Ryan CW, Vasist LS, Van Veldhuizen PJ Jr, Dakhil SR, Lara PN Jr, Drelichman A, Hussain MH, Crawford ED.Clin Genitourin Cancer. 2008 Sep;6(2):103-9. doi: 10.3816/CGC.2008.n.016. PMID: 18824433 </br>10:A Bayesian population PK-PD model for ispinesib/docetaxel combination-induced myelosuppression. Kathman SJ, Williams DH, Hodge JP, Dar M.Cancer Chemother Pharmacol. 2009 Feb;63(3):469-76. doi: 10.1007/s00280-008-0760-4. Epub 2008 Apr 29. PMID: 18443793 |
