A pan-FGFR tyrosine kinase inhibitor with IC50 values of 1.2

JNJ-42756493 – 10 mg

Brand:
Cayman
CAS:
1346242-81-6
Storage:
-20
UN-No:
De Minimis - 3077 / 9

JNJ-42756493 is an orally bioavailable inhibitor of fibroblast growth factor receptor (FGFR) with IC50 values of 1.2, 2.5, 3, and 5.7 nM for FGFR1-4, respectively, using isolated recombinant FGFR kinases.{34449} It is selective for FGFR over the VEGF receptor 2 (IC50 = 36.8 nM). It inhibits proliferation in Ba/F3 cells expressing FGFR subtypes with IC50 values of 22.1, 13.2, and 25 nM for FGFR1, 3, and 4, respectively. It inhibits FGFR activity in non-tumor and tumor cell lines, as well as in xenograft models.{34449} Formulations containing JNJ-42756493 are in Phase II clinical trials for patients with various cancers.  

 

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Description

A pan-FGFR tyrosine kinase inhibitor with IC50 values of 1.2, 2.5, 3, and 5.7 nM for FGFR1-4, respectively, using isolated recombinant FGFR kinases; inhibits proliferation in Ba/F3 cells expressing FGFR subtypes with IC50 values of 22.1, 13.2, and 25 nM for FGFR1, 3, and 4, respectively; has inhibitory activity in vitro and in xenograft models

Formal name: N1-(3,5-dimethoxyphenyl)-N2-(1-methylethyl)-N1-[3-(1-methyl-1H-pyrazol-4-yl)-6-quinoxalinyl]-1,2-ethanediamine

Synonyms:  Erdafitinib

Molecular weight: 446.5

CAS: 1346242-81-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|FGFR Family||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cell Biology|Cell Signaling|Growth Factor Receptors

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