CNX-774( CNX774 | CNX 774 | CNX-774 )

Catalog No. M17187 CAS No. 1202759-32-7

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Product Name

CNX-774
Note

Research use only, not for human use.
Brief Description

CNX-774 is a highly specific, irreversible, and orally active BTK inhibitor (IC50<1 nM).
Description

CNX-774 is a potent Btk inhibitor (IC50 < 1 nM). Recently Bruton's tyrosine kinase (BTK) , a crucial terminal kinase enzyme in the B-cell antigen receptor (BCR) signaling pathway, has emerged as an attractive target for therapeutic intervention in human malignancies and autoimmune disorders.
In Vitro

CNX-774 strongly inhibits Btk activity in Ramos cells with an IC50 of 1-10 nM. CNX-774 demonstrates strong time- and dose-dependent occupancy of Btk in Ramos cells.
In Vivo

CNX-774 is stable and non-reactive in fresh human and rat whole blood and does not covalently bond to any of the mid-level abundance human plasma proteins.CNX-774 demonstrates potent inhibitory activity towards the intended target, Btk, while achieving remarkable specificity in a variety of assays designed to assess off-target reactivity towards abundant cellular thiols and blood proteins.
Synonyms

CNX774 | CNX 774 | CNX-774
Pathway

Apoptosis
Target

Apoptosis
Recptor

BTK
Research Area

Cancer
Indication

——

CAS Number

1202759-32-7
Formula Weight

499.5
Molecular Formula

C26H22FN7O3
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 45 mg/mL. 90.09 mM
SMILES

c1c(ccc(c1)Oc1ccnc(c1)C(=O)NC)Nc1nc(c(cn1)F)Nc1cccc(c1)NC(=O)C=C
Chemical Name

4-(4-((4-((3-acrylamidophenyl)amino)-5-fluoropyrimidin-2-yl)amino)phenoxy)-N-methylpicolinamide

1. Labenski M. 17th North Am Meet Int Soc Study Xenobiot (ISSX) 2011. Abst. P211.

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