1407966-77-1 Usage
Description
PF 06465469, also known as (R)-3-[1-(1-Acryloylpiperidin-3-yl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-N-(4-isopropyl-5-methylphenyl)benzamide, is a covalent inhibitor of Interleukin-2 Inducible T Cell Kinase (Itk) with nanomolar potency in a whole-blood assay. Itk is a member of the TEC-kinase family and is associated with the induction of T cell proliferation and drives cytokines through NFATc. PF 06465469 is a beige solid.
Uses
1. Used in Pharmaceutical Industry:
PF 06465469 is used as a covalent inhibitor for Itk, which plays a role in T cell proliferation and cytokine induction. This application is significant in the development of potential treatments for conditions involving abnormal T cell activity.
2. Used in Research and Development:
PF 06465469 can be utilized in research and development for understanding the role of Itk in immune responses and its potential as a therapeutic target for various diseases.
3. Used in Drug Discovery:
As a potent inhibitor of Itk, PF 06465469 can be employed in drug discovery processes to identify new compounds with similar or improved properties for the treatment of T cell-related disorders.
Check Digit Verification of cas no
The CAS Registry Mumber 1407966-77-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,0,7,9,6 and 6 respectively; the second part has 2 digits, 7 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1407966-77:
(9*1)+(8*4)+(7*0)+(6*7)+(5*9)+(4*6)+(3*6)+(2*7)+(1*7)=191
191 % 10 = 1
So 1407966-77-1 is a valid CAS Registry Number.
1407966-77-1Relevant articles and documents
Covalent inhibitors of interleukin-2 inducible T cell kinase (ItK) with nanomolar potency in a whole-blood assay
Zapf, Christoph W.,Gerstenberger, Brian S.,Xing, Li,Limburg, David C.,Anderson, David R.,Caspers, Nicole,Han, Seungil,Aulabaugh, Ann,Kurumbail, Ravi,Shakya, Subarna,Li, Xin,Spaulding, Vikki,Czerwinski, Robert M.,Seth, Nilufer,Medley, Quintus G.
, p. 10047 - 10063 (2013/01/16)
We wish to report a strategy that targets interleukin-2inducible T cell kinase (Itk) with covalent inhibitors. Thus far, covalent inhibition of Itk has not been disclosed in the literature. Structure-based drug design was utilized to achieve low nanomolar potency of the disclosed series even at high ATP concentrations. Kinetic measurements confirmed an irreversible binding mode with off-rate half-lives exceeding 24 h and moderate on-rates. The analogues are highly potent in a cellular IP1 assay as well as in a human whole-blood (hWB) assay. Despite a half-life of approximately 2 h in resting primary T cells, the covalent inhibition of Itk resulted in functional silencing of the TCR pathway for more than 24 h. This prolonged effect indicates that covalent inhibition is a viable strategy to target the inactivation of Itk.
