1228960-69-7 Usage
Biological Activity
mln0905 is a potent inhibitor of plk1 with ic50 value ranges from 3 to 24 nm [1].polo-like kinase 1 (plk1) is a family of conserved serine/threonine kinases and plays an important role in regulating cell cycle. it has been revealed that plk1 drives cell cycle progression by triggerting g2/m transition and is considered as a pro-oncogene which overexpressed in tumor cells [2].mln0905 is a selective plk1 inhibitor and has similar effect as rnai hnockdown. when tested with ht-29 cells, mln0905 treatment significantly increased phish3 expression which indicated that cells were arrested in g2/m phase by inhibiting plk1 expression [1].in mouse model with human diffuse large b-cell lymphoma (dlbcl) cell line ocily-19 subcutaneous xenograft, co-administration of mln0905 and rituximab markedly reduced tumor volume and increased survival time through inhibiting plk1 which resulted in mitotic arrest [1]. and the same result was achieved when using nude mice model with human colon tumor ht29 xenograft, mln0905 treatment significantly inhibited tumor growth or progression [3].
references
[1]. shi, j.q., et al., mln0905, a small-molecule plk1 inhibitor, induces antitumor responses in human models of diffuse large b-cell lymphoma. mol cancer ther, 2012. 11(9): p. 2045-53.[2]. espeut, j., et al., natural loss of mps1 kinase in nematodes uncovers a role for polo-like kinase 1 in spindle checkpoint initiation. cell rep, 2015. [3]. duffey, m.o., et al., discovery of a potent and orally bioavailable benzolactam-derived inhibitor of polo-like kinase 1 (mln0905). j med chem, 2012. 55(1): p. 197-208.
Check Digit Verification of cas no
The CAS Registry Mumber 1228960-69-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,2,8,9,6 and 0 respectively; the second part has 2 digits, 6 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1228960-69:
(9*1)+(8*2)+(7*2)+(6*8)+(5*9)+(4*6)+(3*0)+(2*6)+(1*9)=177
177 % 10 = 7
So 1228960-69-7 is a valid CAS Registry Number.
1228960-69-7Relevant articles and documents
Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of polo-like kinase 1 (MLN0905)
Duffey, Matthew O.,Vos, Tricia J.,Adams, Ruth,Alley, Jennifer,Anthony, Justin,Barrett, Cynthia,Bharathan, Indu,Bowman, Douglas,Bump, Nancy J.,Chau, Ryan,Cullis, Courtney,Driscoll, Denise L.,Elder, Amy,Forsyth, Nancy,Frazer, Jonathan,Guo, Jianping,Guo, Luyi,Hyer, Marc L.,Janowick, David,Kulkarni, Bheemashankar,Lai, Su-Jen,Lasky, Kerri,Li, Gang,Li, Jing,Liao, Debra,Little, Jeremy,Peng, Bo,Qian, Mark G.,Reynolds, Dominic J.,Rezaei, Mansoureh,Scott, Margaret Porter,Sells, Todd B.,Shinde, Vaishali,Shi, Qiuju Judy,Sintchak, Michael D.,Soucy, Francois,Sprott, Kevin T.,Stroud, Stephen G.,Nestor, Michelle,Visiers, Irache,Weatherhead, Gabriel,Ye, Yingchun,Damore, Natalie
supporting information; experimental part, p. 197 - 208 (2012/03/10)
This article describes the discovery of a series of potent inhibitors of Polo-like kinase 1 (PLK1). Optimization of this benzolactam-derived chemical series produced an orally bioavailable inhibitor of PLK1 (12c, MLN0905). In vivo pharmacokinetic-pharmacodynamic experiments demonstrated prolonged mitotic arrest after oral administration of 12c to tumor bearing nude mice. A subsequent efficacy study in nude mice achieved tumor growth inhibition or regression in a human colon tumor (HT29) xenograft model.
