CNX-774

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CNX-774 是一种高度特异性、不可逆、口服活性的 BTK 抑制剂 (IC50<1 nM)。

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.

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.

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.

CNX774 | CNX 774 | CNX-774

Apoptosis

Apoptosis

BTK

Cancer

——

1202759-32-7

499.5

C26H22FN7O3

>98% (HPLC)

DMSO : ≥ 45 mg/mL. 90.09 mM

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

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

(-20℃)

With Ice Pack

≥ 2 years