881202-45-5 Usage
Uses
JNJ 26854165 is a p53 activator and HDM2 ubiquitin ligase (MDM2) inhibitor.
Biological Activity
jnj-26854165, also named as serdemetan, is originally developed as an activator of p53, is now regarded as a novel oral human double minute-2 (hdm-2) ubiquitin ligase antagonist. it can increase the level of hdm-2 client proteins, such as p53, by inhibiting the association of hdm-2-client protein complex with the proteosome. it is demonstrated potent anti-proliferative and apoptosis-inducing activity of jnj-26854165 in a broad range of p53 wild type and mutant tumor models. in vivo, jnj-26854165 may induce important differences in efs distribution when comparing to control in 18 of 37 solid tumors and in 5 of 7 of the evaluable all xenografts.j. tabernero, l. dirix, p. schoffski, a. cervantes, j. capdevila, j. baselga, l. van beijsterveldt, h. winkler, s. kraljevic and s. h. zhuang. phase i pharmacokinetic (pk) and pharmacodynamic (pd) study of hdm-2 antagonist jnj-26854165 in patients with advanced refractory solid tumors. journal of clinical oncology (meeting abstracts) may 2009 vol. 27 no. 15s 3514malcolm a. smith, richard gorlick, e. anders kolb, richard lock, hernan carol, john m. maris, stephen t. keir, christopher l. morton, c. patrick reynolds, min h. kang, janine arts, tarig bashir, michel janicot, raushan t. kurmasheva, peter j. houghton. initial testing of jnj-26854165 (serdemetan) by the pediatric preclinical testing program. pediatric blood & cancer. volume 59, issue 2, pages 329–332, august 2012.
Check Digit Verification of cas no
The CAS Registry Mumber 881202-45-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,8,1,2,0 and 2 respectively; the second part has 2 digits, 4 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 881202-45:
(8*8)+(7*8)+(6*1)+(5*2)+(4*0)+(3*2)+(2*4)+(1*5)=155
155 % 10 = 5
So 881202-45-5 is a valid CAS Registry Number.
881202-45-5Relevant academic research and scientific papers
INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53
-
Page/Page column 82, (2010/10/20)
The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, X, Y, Q and Z have defined meanings.
