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product name CNX-774


Description: CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 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 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.

References: 17th North Am Meet Int Soc Study Xenobiot.



Molecular Weight (MW)

499.5
Formula

C26H22FN7O3
CAS No.

1202759-32-7
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 100 mg/mL (200.2 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (4.0 mM)
Solubility (In vivo)

 
Synonyms

 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19401373

In Vitro

In vitro activity: In cellular assays, CNX-774 demonstrates potent inhibitory activity towards BTK with IC50 of 1-10 nM by targeting Cys-481 residue within the ATP binding site of the enzyme.


Kinase Assay:


Cell Assay:

In Vivo  
Animal model  
Formulation & Dosage  
References  

Entrectinib

Share this post on:

Author: Sodium channel

Share this post on:

product name CNX-774


Description: CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 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 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.

References: 17th North Am Meet Int Soc Study Xenobiot.



Molecular Weight (MW)

499.5
Formula

C26H22FN7O3
CAS No.

1202759-32-7
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 100 mg/mL (200.2 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (4.0 mM)
Solubility (In vivo)

 
Synonyms

 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19401373

In Vitro

In vitro activity: In cellular assays, CNX-774 demonstrates potent inhibitory activity towards BTK with IC50 of 1-10 nM by targeting Cys-481 residue within the ATP binding site of the enzyme.


Kinase Assay:


Cell Assay:

In Vivo  
Animal model  
Formulation & Dosage  
References  

Entrectinib

Share this post on:

Author: Sodium channel