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CNX-774
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
CNX-774图片
CAS NO:1202759-32-7
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
CNX-774 是一种具有口服活性、不可逆和选择性的 BTK 抑制剂，IC50< 1 nM。 CNX-774 专门针对 Btk 的半胱氨酸 481 进行共价修饰。
Cas No.1202759-32-7
化学名4-[4-[[5-fluoro-4-[3-(prop-2-enoylamino)anilino]pyrimidin-2-yl]amino]phenoxy]-N-methylpyridine-2-carboxamide
Canonical SMILESCNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)F
分子式C26H22FN7O3
分子量499.5
溶解度DMF: 30 mg/ml,DMF:PBS(pH 7.2)(1:6): 0.14 mg/ml,DMSO: 25 mg/ml
储存条件Store at -20° C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

CNX-774 is an orally active and selective inhibitor of BTK with IC50 value of<1 nM.

Bruton’s tyrosine kinase (BTK) is an important enzyme in the B-cell antigen receptor (BCR) signaling pathway and also plays an important role in mast cell activation and B cell maturation.

CNX-774 is an orally active, irreversible and selective BTK inhibitor with IC50 value of<1 nM. CNX-774 formed covalent bond with the Cys481 residue within the ATP binding site of BTK. In cellular assays, CNX-774 inhibited BTK with IC50 values of 1-10 nM [1].

Reference:
[1].  Akinleye A, Chen Y, Mukhi N, et al. Ibrutinib and novel BTK inhibitors in clinical development. J Hematol Oncol, 2013, 6: 59.