egfr mutant in 1 — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T11164	EGFR mutant-IN-1		EGFR
	EGFR mutant- in-1, A 5-methylpyrimidopyridone derivative are effective selective EGFRL858R/T790M/C797S mutant inhibitors with IC50 of 27.5 nM, which significantly weakened EGFRWT effect.		EGFR
T11157L	EGFR-IN-1 hydrochloride		EGFR
	EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride exhibits potent antitumor and antiproliferative activity...		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
T10534	BI-4020		EGFR
	BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. BI-4020 exhibits activity agains the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the d...		EGFR
T61016	EMI1		EGFR
	EMI1 can be used in the mutant EGFR-associated, drug-resistant non-small-cell lung cancer(NSCLC) research. EMI1 is an inhibitor of EGFR L858R/T790M/C797S and EGFR ex19del/T790M/C797S [1].		EGFR
T11157	EGFR-IN-1		EGFR
	EGFR-IN-1, an orally active and irreversible selective inhibitor targeting L858R/T790M mutant EGFR, exhibits strong antiproliferative and antitumor activity, particularly against H1975 cells and first line mutant HCC827 ...		EGFR
T75261	EGFR-IN-1 TFA
	EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR . EGFR-I...
T74561	JBJ-09-063 TFA
	JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor, displaying IC50 values of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R/T790M, 0.083 nM for EGFR L858R/T790M/C797S, and 0.396 nM for EGFR L747S mutations...
T74351	PROTAC EGFR degrader 3		PROTACs
	PROTAC EGFR Degrader 3, a highly potent molecule, exhibits remarkable cellular activity against H1975 and HCC827 cells, maintaining high selectivity. It additionally reveals the lysosome's crucial role in the degradation...		PROTACs
T77073	Losatuxizumab
	Losatuxizumab (ABT-806), an anti-EGFR monoclonal antibody, exhibits selective binding affinity towards various EGFR forms, with EC50 values of 0.96 nM for the wild-type EGFR, 0.09 nM for the C271A,C283A mutant, 0.12 nM f...
T79775	EGFR-IN-89		EGFR
	EGFR-IN-89 (compound 13k) is a fourth-generation inhibitor selectively targeting EGFR mutations, exhibiting potent activity with an IC50 of 10.1 nM against Del19/T790M/C797S mutations, and demonstrating greater selectivi...		EGFR
T79461	YK-029A		EGFR
	YK-029A, an orally active EGFR mutant inhibitor, targets both EGFR T790M and EGFRex20ins mutations. It demonstrates notable antitumor efficacy, inducing tumor regression in EGFRex20ins-driven patient-derived xenograft (P...		EGFR
T74633	MS9427
	MS9427 is a potent PROTAC EGFR degrader, demonstrating high affinity for EGFR with dissociation constants (K d s) of 7.1 nM for the wild-type (WT) EGFR and 4.3 nM for the L858R mutant EGFR, indicating selective degradati...
T80748	YS-363		EGFR
	YS-363 is a potent, selective, and orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting half-maximal inhibitory concentrations (IC50) of 0.96 nM for the wild-type EGFR and 0.67 nM for the ...		EGFR
T74635	MS9449		PROTACs
	MS9449 is a potent PROTAC EGFR degrader, exhibiting dissociation constants (Kd) of 17 nM for EGFR WT and 10 nM for EGFR L858R. It effectively mediates the degradation of mutant EGFRs via both ubiquitin/proteasome system ...		PROTACs
T35897	ASK120067
	ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]...
T74634	MS9427 TFA		PROTACs
	MS9427 TFA is a potent PROTAC-based EGFR degrader, exhibiting dissociation constants (Kd) of 7.1 nM for wild-type EGFR and 4.3 nM for the L858R EGFR mutation. It preferentially degrades the mutant EGFR, sparing the wild-...		PROTACs