CNX-774 - CAS 1202759-32-7
Catalog number: 1202759-32-7
Category: Inhibitor
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Molecular Formula:
C26H22FN7O3
Molecular Weight:
499.49638
COA:
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Targets:
BTK
Description:
CNX-774 is a potent Btk inhibitor (IC50 < 1 nM)
Synonyms:
CNX-774; CNX 774; CNX774.
MSDS:
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InChIKey:
VVLHQJDAUIPZFH-UHFFFAOYSA-N
InChI:
InChI=1S/C26H22FN7O3/c1-3-23(35)31-17-5-4-6-18(13-17)32-24-21(27)15-30-26(34-24)33-16-7-9-19(10-8-16)37-20-11-12-29-22(14-20)25(36)28-2/h3-15H,1H2,2H3,(H,28,36)(H,31,35)(H2,30,32,33,34)
Canonical SMILES:
CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)F
Current Developer:
Avila Therapeutics
1.BTK inhibition is a potent approach to block IgE-mediated histamine release in human basophils.
Smiljkovic D;Blatt K;Stefanzl G;Dorofeeva Y;Skrabs C;Focke-Tejkl M;Sperr WR;Jaeger U;Valenta R;Valent P Allergy. 2017 Nov;72(11):1666-1676. doi: 10.1111/all.13166. Epub 2017 Apr 20.
BACKGROUND: ;Recent data suggest that Bruton's tyrosine kinase (BTK) is an emerging therapeutic target in IgE receptor (IgER)-cross-linked basophils.;METHODS: ;We examined the effects of four BTK inhibitors (ibrutinib, dasatinib, AVL-292, and CNX-774) on IgE-dependent activation and histamine release in blood basophils obtained from allergic patients (n=11) and nonallergic donors (n=5). In addition, we examined the effects of these drugs on the growth of the human basophil cell line KU812 and the human mast cell line HMC-1.;RESULTS: ;All four BTK blockers were found to inhibit anti-IgE-induced histamine release from basophils in nonallergic subjects and allergen-induced histamine liberation from basophils in allergic donors. Drug effects on allergen-induced histamine release were dose dependent, with IC;50; values ranging between 0.001 and 0.5 μmol/L, and the following rank order of potency: ibrutinib>AVL-292>dasatinib>CNX-774. The basophil-targeting effect of ibrutinib was confirmed by demonstrating that IgE-dependent histamine release in ex vivo blood basophils is largely suppressed in a leukemia patient treated with ibrutinib. Dasatinib and ibrutinib were also found to counteract anti-IgE-induced and allergen-induced upregulation of CD13, CD63, CD164, and CD203c on basophils, whereas AVL-292 and CNX-774 showed no significant effects.
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CAS 1202759-32-7 CNX-774

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