Erdafitinib (JNJ-42756493) (C09-0880-928)

InformationErdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, panfibroblast growth factor receptor (FGFR)inhibitor with potential antineoplastic activity. Erdafitinib also binds toRET (c-RET),CSF-1R,PDGFR-α/PDGFR-β,FLT4,Kit (c-Kit)andVEGFR-2and induces cellularapoptosis.TargetsFGFR ; RET ; CSF-1R ; PDGFR ; Kit 16439,In vitroJNJ-42756493 is a potent, oral pan-FGFR tyrosine kinase inhibitor with half-maximal inhibitory concentration values in the low nanomolar range for all members of the FGFR family (FGFR1 to FGFR4), with minimal activity on vascular endothelial growth factor receptor (VEGFR) kinases compared with FGFR kinases (approximately 20-fold potency difference). the proliferation of cells treated with JNJ-42756493 is decreased, associated with increased apoptotic death and decreased cell survival.In vivogrowth of NCI-H716 tumors is delayed by 5 days by drug treatment alone, although when drug delivery is stopped the relative tumor volume increased compared to control. JNJ-42756493 shows favorable drug like properties and displays a high distribution to lung, liver and kidney tissue. JNJ-42756493 is well tolerated at efficacious doses and results in potent dose-dependent antitumor activity accompanied by pharmacodynamic modulation of tumor FGFR and downstream pathway components.Cell Research(from reference)Cell lines：HCT116, HCA7, Caco2 and NCI-H716 cells Incubation Time：72 h. Specification: 0.975 Molecular Formula: C25H30N6O2 Molecular Weight: 446.54 EC Number: 807-395-6 PubChem CID: 67462786 Isomeric SMILES: CC(C)NCCN(C1=CC2=NC(=CN=C2C=C1)C3=CN(N=C3)C)C4=CC(=CC(=C4)OC)OC Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/E414001-SCI_146e7ddd11c6e456942db7de3a5f03b3.pdf