l858r — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T74833	EGFR T790M/L858R-IN-2
	EGFRT790M/L858R-IN-2 is a potent, selective inhibitor of EGFRT790M/L858R, exhibiting IC50 values of 3.5 nM for EGFRT790M/L858R and 1290 nM for EGFR WT. This compound effectively decreases the expression of p-EGFR, P-AKT,...
T5462	Almonertinib	HS-10296	EGFR
	Almonertinib (HS-10296) is an inhibitor of EGFR activation mutation and tolerant mutation of EGFR T790M, which has only limited activity against wild-type EGFR.		EGFR
T5675	Almonertinib hydrochloride	HS-10296 hydrochloride	EGFR
	Almonertinib hydrochloride (HS-10296 hydrochloride) is a small molecule inhibitor of EGFR-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.		EGFR
T11160	EGFR-IN-5		EGFR
	EGFR-IN-5 is a selective inhibitor of EGFR. The IC50s for EGFR, EGFR(L858R), EGFR(L858R/T790M), and EGFR(L858R/T790M/C797S) are 10.4, 1.1, 34, 7.2 nM, respectively.		EGFR
T3634	Osimertinib mesylate	Mereletinib mesylate,AZD-9291 mesylate	EGFR
	Osimertinib mesylate (Mereletinib mesylate) is an irreversible and mutant selective EGFR inhibitor (IC50s: 12/1 nM for EGFR(L858R) and EGFR(L858R/T790M)).		EGFR
T2303	(S)-Afatinib	BIBW2992	EGFR , HER
	(S)-Afatinib (BIBW2992) is an irreversible EGFR family inhibitor with IC50s of 0.5/0.4/10/14/1 nM for EGFRwt, EGFR (L858R), EGFR (L858R/T790M), HER2, and HER4, respectively.		EGFR , HER
T10419	AV-412	MP412	EGFR
	AV-412 (MP412) is an EGFR inhibitor (EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M and ErbB2 with IC50s of 0.75, 0.79, 0.5, 2.3, 19 nM).		EGFR
T6238	WZ4002		EGFR
	WZ4002 is a mutant-selective EGFR inhibitor for EGFR(L858R) and EGFR(T790M) with IC50 of 2 nM/8 nM.		EGFR
T21322	Mavelertinib	PF 06747775,PFE-X775,PF-06747775,PF-7775,PF 6747775,PF6747775	EGFR
	Mavelertinib (PF-06747775) is an orally available, selective and potent EGFR tyrosine kinase (EGFR TKI) inhibitor with inhibitory effects on T790M/L858R and T790M/Del, and can be used in the study of oncology and respira...		EGFR
T6733	WZ-3146		EGFR
	WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).		EGFR
T21312	Afatinib	Afatinib free base,BIBW 2992	EGFR , Autophagy
	Afatinib (BIBW 2992) is an irreversible inhibitor of EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M and HER2 with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM , respectively).		EGFR , Autophagy
T4249	AZD3759 hydrochloride		EGFR
	AZD3759 (hydrochloride) is an effective, orally active and central nervous system-penetrant EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.2/0.3/0.2 nM for EGFR (L858R)/EGFR (wt)/EGFR (exon 19Del).		EGFR
T7322	Theliatinib		EGFR
	Theliatinib, a potent and highly selective EGFR inhibitor, with anti-tumor activity. Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively.		EGFR
T11163	EGFR-IN-9		EGFR
	EGFR-IN-9 is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity.		EGFR
T22272	Lifirafenib	BGB-283,Beigene-283	EGFR , Raf
	Lifirafenib (Beigene-283) is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant respective...		EGFR , Raf
T5437	Gefitinib-based PROTAC 3		EGFR
	Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectivel...		EGFR
T60076	Oritinib	SH-1028	EGFR
	Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (d746-750), EGFR (d746-750/T790M), respectively. Oritinib can ...		EGFR
T4485	Lazertinib	Lazertinib (YH25448),GNS-1480,YH25448	EGFR
	Lazertinib (GNS-1480) is an effective, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively...		EGFR
T2705	Mutant EGFR inhibitor		EGFR
	Mutant EGFR inhibitor is a selective and potent Mutated EGFR inhibitor, inhibits L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant.		EGFR
T16162	Mutated EGFR-IN-1	Osimertinib analog	EGFR
	Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant, and T790M resistance mutant.		EGFR