CNX-774

Catalog No.S7257

CNX-774 Chemical Structure

Molecular Weight(MW): 499.5

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

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1 Customer Review

  • Effects of AVL-292, CNX-774 and dasatinib on IgE-mediated histamine release in human basophils. Basophils (BA) obtained from three nonallergic donors (A), three patients allergic to Der p 2, and three patients allergic to Phl p 5 (B and C) were preincubated in control medium (Co) or medium containing various concentrations of AVL-292, CNX-774, or dasatinib (0.001-1 μmol/L) at 37°C for 30 minutes. Then, cells were exposed to anti-IgE antibody E-124.2.8 (1 μg/mL; nonallergic donors) or recombinant allergens (1 μg/mL of rDer p 2 or rPhl p 5 in allergic patients) at 37°C for 30 minutes. After centrifugation, histamine concentrations were determined in cell-free supernatants and cell lysates. Histamine release is expressed as percentage of total histamine. Results show the percentage of control and represent mean SD from three independent experiments (three donors). Asterisk (*): P<0.05 by Student's t test with Bonferroni correction

    Allergy, 2017. CNX-774 purchased from Selleck.

Purity & Quality Control

Choose Selective BTK Inhibitors

Biological Activity

Description CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM.
Features Orally bioavailable BTK-selective inhibitor, binding covalently to target protein.
Targets
BTK [1]
<1 nM
In vitro

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. [1]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (200.2 mM)
Ethanol 2 mg/mL (4.0 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 499.5
Formula

C26H22FN7O3

CAS No. 1202759-32-7
Storage powder
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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BTK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID