An allosteric inhibitor of Bcr-Abl (IC50 = 0.121 µM); inhibits the Bcr-Abl mutants Bcr-AblG250E

GNF-5 – 5 mg

Brand:
Cayman
CAS:
778277-15-9
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

GNF-5 is an allosteric inhibitor of Bcr-Abl (IC50 = 0.121 µM) and a derivative of GNF-2 (Item No. 16253).{61146} It also inhibits the Bcr-Abl mutants Bcr-AblG250E, Bcr-AblE255V, and Bcr-AblM351T (IC50s = 4.52, 0.38, and 0.93 µM, respectively).{30754} GNF-5 inhibits the growth of Ba/F3 cells (IC50 = 0.145 µM).{61146} It reduces viral titers in Vero cells infected with infectious bronchitis virus (IBV), a coronavirus, when used at a concentration of 10 µM via inhibition of IBV surface glycoprotein-induced syncytia formation and virus-cell fusion.{45828} GNF-5 (75 mg/kg) increases survival in a recalcitrant mutant Bcr-AblT315I mouse bone marrow transplantation model when administered alone or in combination with nilotinib.{30754}  

 

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Description

An allosteric inhibitor of Bcr-Abl (IC50 = 0.121 µM); inhibits the Bcr-Abl mutants Bcr-AblG250E, Bcr-AblE255V, and Bcr-AblM351T (IC50s = 4.52, 0.38, and 0.93 µM, respectively); reduces viral titers in IBV-infected Vero cells at 10 µM; increases survival in a recalcitrant mutant Bcr-AblT315I mouse bone marrow transplantation model at 75 mg/kg

Formal name: N-(2-hydroxyethyl)-3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]-benzamide

Synonyms: 

Molecular weight: 418.4

CAS: 778277-15-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Antivirals|Entry/fusion Inhibitors||Product Type|Biochemicals|Kinase Inhibitors|Abl Family & Bcr-Abl||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Abl family & Bcr-Abl Signaling||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Viral Diseases|Coronaviruses

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