Egfr-in-8 is a dual inhibitor of EGFR and c-Met, compound 48. Egfrin-8 is expected to be a target for further development of EGFR TKI resistant NSCLC active molecules.

 

Brand: BCM

 

Target: EGFR; c-Met

 

Signaling Pathways: Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors

 

In Vitro: In A549, PC9, H1975, CL68, and CL97 cells, EGFR-IN-8 (0-0.6 μM; 48 hours) suppresses the expression of EGFR and c-Met in these five cell lines irrespective of their mutational status. EGFR-IN-8 (0-20 μM; 24, 48, 72 hours) exhibits a time- and dose-dependent inhibitory effect on the viability of A549, PC9, H1975, CL68, and CL97 cells at different time intervals, with IC50 values ranging from 0.3 to 0.6 μM and 0.2-0.5 μM after 48 and 72 h of treatment respectively.

 

Solubility: Soluble in DMSO.

 

pKa: 10.78±0.70(Predicted)

 

Isomeric SMILES: C1CC1C(=O)NC2=C(C=C(C=C2)NC(=O)NC3=CC=CC(=C3)C4=NC(=NO4)C5=C(C=C(C=C5)NC(=O)C6=CN=CC=C6)Cl)C(F)(F)F  

 

InChIKey: IIUNSVLRVWGJRM-UHFFFAOYSA-N  

 

InChI: InChI=1S/C32H23ClF3N7O4/c33-25-15-22(38-29(45)19-4-2-12-37-16-19)8-10-23(25)27-42-30(47-43-27)18-3-1-5-20(13-18)39-31(46)40-21-9-11-26(24(14-21)32(34,35)36)41-28(44)17-6-7-17/h1-5,8-17H,6-7H2,(H,38,45)(H,41,44)(H2,39,40,46)

 

Attribute
[Chem Name]	N-[3-chloro-4-[5-[3-[[4-(cyclopropanecarbonylamino)-3-(trifluoromethyl)phenyl]carbamoylamino]phenyl]-1,2,4-oxadiazol-3-yl]phenyl]pyridine-3-carboxamide
[Synonym]	EGFR-IN-8
[CAS No.]	2407957-87-1
[MDL No.]	MFCD32201095
[Formula]	C32H23ClF3N7O4
[Molecular]	662.02
[Form]	Light yellow to yellow solid
[Storage]	Sealed in dry, 2-8°C

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