1234480-46-6 Usage
Description
XMD8-87 is an inhibitor of tyrosine kinase non-receptor 2 (TNK2) with an IC50 value of 1.9 μM in HEK293T cells expressing human TNK2. It is selective for TNK2 over a panel of approximately 100 kinases with >90 and <50% inhibition for TNK2 and all other kinases tested, respectively. XMD8-87 inhibits growth of Ba/F3 cells expressing constitutively active mutant TNK2s (IC50s = 0.1-77 nM) commonly found in leukemias but has no effect on cells expressing wild-type TNK2 (IC50 = >1 μM).
Uses
XMD8-87 is used in the studies of benzopyrimidodiazepinones as most selective and potent ERK5 inhibitor.
Check Digit Verification of cas no
The CAS Registry Mumber 1234480-46-6 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,3,4,4,8 and 0 respectively; the second part has 2 digits, 4 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1234480-46:
(9*1)+(8*2)+(7*3)+(6*4)+(5*4)+(4*8)+(3*0)+(2*4)+(1*6)=136
136 % 10 = 6
So 1234480-46-6 is a valid CAS Registry Number.
1234480-46-6Relevant articles and documents
Benzopyrimidodiazepinone inhibitors of TNK2
Chen, Bailing,Feru, Frederic,Feutrill, John,Gero, Thomas W.,Gray, Nathanael S.,Groendyke, Brian J.,Li, Bin,Li, Zhengnian,Pang, Kevin,Powell, Chelsea E.,Scott, David A.,Szabo, Hilary
, (2020/01/22)
The SAR of a series of benzopyrimidodiazepinone inhibitors of TNK2 was developed, starting from the potent and selective compound XMD8-87. A diverse set of anilines was introduced in an effort to improve the in vivo PK profile and minimize the risk of quinone diimine formation.
PYRIMIDO-DIAZEPINONE KINASE SCAFFOLD COMPOUNDS AND METHODS OF TREATING DISORDERS
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Page/Page column 54, (2010/08/04)
The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPSl (TTK), ERK5 (BMKl, MAPK7), polo kinase 1,2,3, or 4, Ackl, Ack2, AbI, DCAMKLl, ABLl, AbI mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4,
