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Isoforms Recommended:	EGFR/ErbB1/HER1

Results for "

EGFR L858R-T790M

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (73) Akt (7) Anaplastic lymphoma kinase (ALK) (1) Apoptosis (15) Autophagy (5) Bcl-2 Family (2) BMX Kinase (1) Btk (2) c-Met/HGFR (3) Caspase (1) Drug Derivative (1) ERK (4) HSP (1) Isotope-Labeled Compounds (1) MEK (1) p38 MAPK (4) PARP (1) PROTACs (6) Reference Standards (3) STAT (2) Survivin (1)
By Research Areas:	Cancer (73) Endocrinology (1) Infection (3) Inflammation/Immunology (1) Metabolic Disease (2) Neurological Disease (2)
Click Chemistry:	PROTAC Synthesis (2) Alkynes (3)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: EGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15772

Osimertinib Maximum Cited Publications 185 Publications Verification AZD-9291; Mereletinib	EGFR	Cancer
Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective *EGFR* inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

HY-10261

Afatinib 100+ Cited Publications BIBW 2992	EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK	Cancer
Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC₅₀ values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR ^wt, EGFR ^L858R, EGFR ^L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .

HY-15772A

Osimertinib mesylate Maximum Cited Publications 185 Publications Verification AZD-9291 mesylate; Mereletinib mesylate	EGFR	Cancer
Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective *EGFR* inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

HY-10261A

Afatinib dimaleate 100+ Cited Publications BIBW 2992MA2	EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK	Cancer
Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC₅₀ values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR ^wt, EGFR ^L858R, EGFR ^L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .

HY-B0793

AZ-5104 5+ Cited Publications	EGFR	Cancer
AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an *EGFR* inhibitor with IC₅₀s of 1, 6, 1, 25 and 7 nM for EGFR ^L858R/T790M, EGFR ^L858R, EGFR ^L861Q, EGFR and ErbB4, respectively.

HY-79077

Osimertinib dimesylate Maximum Cited Publications 185 Publications Verification AZD-9291 dimesylate; Mereletinib dimesylate	EGFR	Cancer
Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective *EGFR* inhibitor with IC₅₀s of 12 and 1 nM against EGFR ^L858R and EGFR ^L858R/T790M, respectively.

HY-15772R

Osimertinib (Standard) AZD-9291 (Standard); Mereletinib (Standard)	Reference Standards EGFR	Cancer
Osimertinib (Standard) is the analytical standard of Osimertinib. This product is intended for research and analytical applications. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective *EGFR* inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

HY-15164A

Icotinib 5+ Cited Publications BPI-2009	EGFR	Infection Neurological Disease Metabolic Disease Cancer
Icotinib (BPI-2009) is a potent, CNS-penetrant and specific *EGFR* inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^T790M and EGFR ^L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-N1073

Wighteone 1 Publications Verification 6-Isopentenylgenistein; Erythrinin B	Apoptosis EGFR HSP ERK Akt	Infection Cancer
Wighteone (6-Isopentenylgenistein; Erythrinin B) is a prenylated isoflavone that acts as a HSP90/EGFR ^L858R/T790M inhibitor and antifungal agent. Wighteone reduces the expression level of HSP90, blocks EGF-induced phosphorylation of *EGFR, and thereby inhibits the downstream ERK* and AKT signaling pathways. Wighteone induces cell cycle redistribution, inhibits proliferation and triggers apoptosis in cancer cells. Wighteone can be isolated from Erythrina suberosa, and can also be induced to synthesize in Lotus japonicus under specific conditions. Wighteone can be used to study HER2-positive breast cancer, leukemia, non-small cell lung cancer with EGFR ^L858R/T790M mutation, and fungal infections .

HY-15730

Poziotinib 5+ Cited Publications HM781-36B; NOV120101	EGFR Apoptosis	Cancer
Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFR ^wt, HER-2 and HER-4 with IC₅₀s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFR ^T790M and EGFR ^L858R/T790M, with IC₅₀s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity .

HY-100213

EAI045 3 Publications Verification	EGFR	Cancer
EAI045 is an allosteric and the fourth-generation inhibitor of mutant *EGFR* with IC₅₀s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR ^L858R, EGFR ^T790M and EGFR ^L858R/T790M at 10 μM ATP, respectively.

HY-147858

PROTAC EGFR degrader 7	PROTACs EGFR Apoptosis	Cancer
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR ^L858R/T790M degrader, with a DC₅₀ of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC₅₀ of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-15772S1

Osimertinib-13C,d3 AZD-9291-¹³C,d₃; Mereletinib-¹³C,d₃	EGFR	Cancer
Osimertinib- ¹³C,d₃ is the deuterium and ¹³C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.

HY-10325

CL-387785 2 Publications Verification EKI-785; WAY-EKI 785	EGFR Apoptosis	Endocrinology Cancer
CL-387785 (EKI-785; WAY-EKI 785) is an orally active EGFR inhibitor with an IC₅₀ of 370 pM. CL-387785 inhibits EGF-stimulated EGFR autophosphorylation with an IC₅₀ of approximately 5 nM. CL-387,785 exerts selective inhibition on cell lines overexpressing EGFR or c-erbB-2, whereas it shows weak inhibitory effects on cell lines with low expression of these two receptors. CL-387785 effectively induces cell cycle arrest and apoptosis. CL-387785 can be used for the research of non-small cell lung cancer and autosomal recessive polycystic kidney disease .

HY-12001

WZ-3146	EGFR	Cancer
WZ3146 is a mutant selective *EGFR* inhibitor with IC₅₀s of 2, 2, 5, 14 and 66 nM for EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^E746_A750, EGFR ^{E746_A750/T790M} and EGFR, respectively.

HY-12026

WZ4002 5+ Cited Publications	EGFR	Cancer
WZ4002 is a mutant selective *EGFR* inhibitor with IC₅₀s of 2, 8, 3 and 2 nM for EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^E746_A750 and EGFR ^{E746_A750/T790M}, respectively.

HY-15164

Icotinib Hydrochloride 5+ Cited Publications BPI-2009H	EGFR	Infection Neurological Disease Metabolic Disease Cancer
Icotinib Hydrochloride (BPI-2009) is a potent, CNS-penetrant and specific *EGFR* inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^T790M and EGFR ^L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-132842A

(S)-Sunvozertinib (S)-DZD9008	EGFR Btk	Cancer
(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against *EGFR* exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC₅₀=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK .

HY-135805

JBJ-04-125-02	EGFR	Cancer
JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active *EGFR* inhibitor with an IC₅₀ of 0.26 nM for EGFR ^L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR ^{L858R/T790M/C797S} signaling. JBJ-04-125-02 has anti-tumor activities .

HY-10346

AV-412 5 Publications Verification MP412	EGFR	Cancer
AV-412 (MP412) is an *EGFR* inhibitor with IC₅₀s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR ^L858R, EGFR ^T790M, EGFR ^L858R/T790M and ErbB2, respectively.

HY-111415

EGFR-IN-5	EGFR	Cancer
EGFR-IN-5 is a *EGFR* inhibitor with IC₅₀s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFR ^L858R, EGFR ^L858R/T790M, and EGFR ^{L858R/T790M/C797S}, respectively.

HY-146349

PROTAC EGFR degrader 4	PROTACs EGFR Autophagy	Cancer
PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant *EGFR*.PROTAC EGFR degrader 4 induces EGFR ^del19 and EGFR ^L858R/T790M degradation with DC₅₀s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC₅₀s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy .

HY-15772S

Osimertinib-d6 AZD-9291-d₆; Mereletinib-d₆	EGFR	Cancer
Osimertinib-d₆ is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

HY-139920

Oritinib 1 Publications Verification SH-1028	EGFR	Cancer
Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFR ^WT, EGFR ^L858R, EGFR ^L861Q, EGFR ^L858R/T790M, EGFR ^d746-750 and EGFR ^{d746-750/T790M} kinases, with IC₅₀s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively .

HY-139997

DDC-01-163	PROTACs EGFR	Cancer
DDC-01-163 is an allosteric PROTAC degrader targeting *EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M* (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer .

HY-119944

JND3229 1 Publications Verification	EGFR	Cancer
JND3229 is a reversible EGFR ^C797S inhibitor with IC₅₀ values of 5.8, 6.8 and 30.5 nM for EGFR ^{L858R/T790M/C797S}, EGFR ^WT and EGFR ^L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma .

HY-100214

EAI001	EGFR	Cancer
EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC₅₀ value of 24 nM for EGFR ^L858R/T790M. EAI001 can be used for research of cancer .

HY-147183A

JBJ-09-063 TFA	EGFR	Cancer
JBJ-09-063 TFA is a mutant-selective allosteric *EGFR* inhibitor with IC₅₀s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer .

HY-147183B

JBJ-09-063 hydrochloride	EGFR	Cancer
JBJ-09-063 hydrochloride is a mutant-selective allosteric *EGFR* inhibitor with IC₅₀s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer .

HY-15772AR

Osimertinib mesylate (Standard) AZD-9291 mesylate (Standard); Mereletinib mesylate (Standard)	Reference Standards EGFR	Cancer
Osimertinib (mesylate) (Standard) is the analytical standard of Osimertinib (mesylate). This product is intended for research and analytical applications. Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective *EGFR* inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

HY-147183

JBJ-09-063	EGFR	Cancer
JBJ-09-063 is a mutant-selective allosteric *EGFR* inhibitor with IC₅₀s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .

HY-135914

JBJ-02-112-05	EGFR	Cancer
JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active *EGFR* inhibitor with an IC₅₀ of 15 nM for EGFR ^L858R/T790M .

HY-10346A

AV-412 free base 5 Publications Verification MP-412 free base	EGFR	Cancer
AV-412 free base (MP-412 free base) is an *EGFR* inhibitor with IC₅₀s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR ^L858R, EGFR ^T790M, EGFR ^L858R/T790M and ErbB2, respectively.

HY-128778

Gozanertinib DBPR112	EGFR	Cancer
Gozanertinib is an orally active furanopyrimidine-based *EGFR* inhibitor with IC₅₀s of 15 nM and 48 nM for EGFR ^WT and EGFR ^L858R/T790M, respectively. Gozanertinib can occupy the ATP-binding site. Gozanertinib has significant antitumor efficacy .

HY-171958

PROTAC EGFR degrader 12	PROTACs EGFR	Cancer
PROTAC EGFR degrader 12 (example 1) is a PROTAC degrader targeting *EGFR* that can effectively degrade EGFR mutants, but has little effect on EGFR WT. PROTAC EGFR degrader 12 shows IC_{50_{s against EGFR ^L858R-T790M (NCI-H1975 cells), EGFR ^L858R (NCI-H3255 cells), and EGFR ^{L858R-T790M-L797S} (NCI-H1975+CS cells) of all <50 nM .}}

HY-101522

CHMFL-EGFR-202	EGFR BMX Kinase Btk MEK	Cancer
CHMFL-EGFR-202 is a potent, irreversible inhibitor of *epidermal growth factor receptor (EGFR) mutant kinase, with IC₅₀s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR* T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines .

HY-150905

EGFR ligand-2	EGFR	Cancer
EGFR ligand-2 (compound C4), a covalent *EGFR* ligand, is a EGFR mutant inhibitor with IC₅₀s of 21 nM and 48 nM for EGFR ^L858R and EGFR ^L858R/T790M, respectively. EGFR ligand-2 can be used to synthesize PROTAC .

HY-133780

Afatinib impurity 11	EGFR Autophagy	Cancer
Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible *EGFR* family inhibitor with IC₅₀s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR ^wt, EGFR ^L858R, EGFR ^L858R/T790M and HER2, respectively .

HY-19617A

EGFR-IN-1 hydrochloride	EGFR	Cancer
EGFR-IN-1 hydrochloride is an orally active and irreversible **L858R/T790M mutant selective EGFR** inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .

HY-150610

EGFR-IN-69	EGFR	Cancer
EGFR-IN-69 (compound 17g) is a potent *EGFR* inhibitor, with IC₅₀ values of 4.3, 6.6 and 25.6 nM against EGFR ^{L858R/T790M/C797S}, EGFR ^L858R/T790M, and EGFR ^{19del/T790M/C797S}, respectively. EGFR-IN-69 can be used for non-small-cell-lung-cancer (NSCLC) research .

HY-10261D

Afatinib oxalate BIBW 2992 oxalate	EGFR Autophagy Apoptosis c-Met/HGFR Akt	Cancer
Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC₅₀ values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR ^wt, EGFR ^L858R, EGFR ^L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .

HY-178283

EGFR-IN-177	EGFR	Cancer
EGFR-IN-177 is a potent *EGFR* inhibitor with IC₅₀s of 0.32, 1.04, 0.65, 0.67, 0.48, 0.55 and 0.38 nM against **EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S*, EGFR* D746-750, EGFR D746-750/C797S, EGFR D770_N77linsNPG, and EGFR WT. EGFR-IN-177 inhibits lung cancer proliferation and EGFR phosphorylation. EGFR-IN-177 can be used for the study of cancers such as non-small cell lung cancer .

HY-164392

TAS-121	EGFR Apoptosis	Cancer
TAS-121 is an orally active, selective, covalent, third-generation mutant **EGFR-tyrosine kinase inhibitor (EGFR-TKI)*. TAS-121 inhibits the L858R* mutation (IC₅₀=1.7 nM), Ex19del mutation (IC₅₀=2.7 nM), L858R/T790M mutation (IC₅₀=0.56 nM) and Ex19del/T790M mutation (IC₅₀=1.1 nM) and wild-type EGFR (IC₅₀=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC₅₀s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models .

HY-174293

Osimertinib dimer	Drug Derivative	Cancer
Osimertinib dimer is a dimer of Osimertinib (HY-15772). Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective *EGFR* inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

HY-175864

EGFR-IN-173	EGFR Apoptosis p38 MAPK ERK Akt STAT	Inflammation/Immunology Cancer
EGFR-IN-173 is an orally active, pan-mutant *EGFR* tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR ^{19del/T790M/C797S} with an IC₅₀ of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC₅₀ = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research .

HY-151981

EGFR-IN-74	EGFR	Cancer
EGFR-IN-74 (Compound 21) is a potent *EGFR* inhibitor with an IC₅₀ of 138 nM against EGFR L858R/T790M. EGFR-IN-74 induces cancer cell apoptosis .

HY-18213

EGFR-IN-9	EGFR	Cancer
EGFR-IN-9 (Compound 8) 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 .

HY-146132

EGFR-IN-55	EGFR	Cancer
EGFR-IN-55 (Compound 8a) is a potent *EGFR* inhibitor with IC₅₀ values of 70 nM and 3.9 nM against EGFR ^WT and EGFR ^L858R/T790M, respectively. EGFR-IN-55 arrests NCI-H1975 cells in G0/G1 phase and shows anticancer activity .

HY-163396

EGFR-IN-107	EGFR Apoptosis	Cancer
EGFR-IN-107 (compound 3r) is an orally active *EGFR* inhibitor with IC₅₀ values of 0.4333 μM for EGFR ^WT and 0.0438 μM for EGFR ^L858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research .

HY-155118

EGFR-IN-81	EGFR	Cancer
EGFR-IN-81 (Compound 10i) is an *EGFR* inhibitor. EGFR-IN-81 inhibits EGFR WT and L858R/T790M with IC₅₀s 4.38 nM and 5.69 nM. EGFR-IN-81 has cytotoxic activity against MCF-7 and HCT116 cells with of 2.07 μM and 6.72 μM respectively .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N1073

Wighteone 1 Publications Verification 6-Isopentenylgenistein; Erythrinin B	Leguminosae Genista ephedroides DC. Plants Isoflavones Source Classification	Apoptosis EGFR HSP ERK Akt
Wighteone (6-Isopentenylgenistein; Erythrinin B) is a prenylated isoflavone that acts as a HSP90/EGFR ^L858R/T790M inhibitor and antifungal agent. Wighteone reduces the expression level of HSP90, blocks EGF-induced phosphorylation of *EGFR, and thereby inhibits the downstream ERK* and AKT signaling pathways. Wighteone induces cell cycle redistribution, inhibits proliferation and triggers apoptosis in cancer cells. Wighteone can be isolated from Erythrina suberosa, and can also be induced to synthesize in Lotus japonicus under specific conditions. Wighteone can be used to study HER2-positive breast cancer, leukemia, non-small cell lung cancer with EGFR ^L858R/T790M mutation, and fungal infections .

Cat. No.	Product Name	Chemical Structure

HY-15772S1

Osimertinib-13C,d3
Osimertinib- ¹³C,d₃ is the deuterium and ¹³C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.

HY-15772S

Osimertinib-d6
Osimertinib-d₆ is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

HY-15164AS

Icotinib-d4

Icotinib-d₄ is the deuterium-labeled Icotinib (HY-15164A). Icotinib-d₄ (BPI-2009) is a potent and specific EGFR inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^T790M and EGFR ^L861Q. Icotinib-d₄ is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Cat. No.	Product Name		Classification

HY-15164A

Icotinib 5+ Cited Publications BPI-2009		Alkynes
Icotinib (BPI-2009) is a potent, CNS-penetrant and specific *EGFR* inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^T790M and EGFR ^L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-147858

PROTAC EGFR degrader 7		Alkynes PROTAC Synthesis
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR ^L858R/T790M degrader, with a DC₅₀ of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC₅₀ of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-15164

Icotinib Hydrochloride 5+ Cited Publications BPI-2009H		Alkynes
Icotinib Hydrochloride (BPI-2009) is a potent, CNS-penetrant and specific *EGFR* inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^T790M and EGFR ^L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-153605

EGFR-IN-77		PROTAC Synthesis
EGFR-IN-77 (Compound 4a) is a selective EGFR ^T790M/L858R inhibitor, with an IC₅₀ of 0.101 μM against *EGFR* ^T790M/L858R, 0.477 μM against *EGFR* ^L858R, and 1.771 μM against wild-type *EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFR* ^T790M/L858R non-small cell lung cancer. EGFR-IN-77 can be used for the research of *EGFR* ^L858R/T790M double-mutant non-small cell lung cancer .

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