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Isoforms Recommended:	EGFR/ErbB1/HER1

Results for "

EGFR(WT)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (48) Akt (3) Apoptosis (15) Autophagy (6) Bcl-2 Family (1) Btk (1) c-Met/HGFR (5) Caspase (1) CDK (1) Isotope-Labeled Compounds (1) p38 MAPK (4) PROTACs (4) Raf (1)
By Research Areas:	Cancer (49)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: EGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-156912

Tyrosine kinase-IN-7	EGFR	Cancer
Tyrosine kinase-IN-7 (compound 13h) is an inhibitor of the tyrosine kinase EGFR. The IC₅₀s for inhibiting EGFR(WT) and EGFR(T790M) are 0.630 μM and 0.956 μM respectively. Tyrosine kinase-IN-7 has antitumor activity against four cancer cell lines (HepG2, HCT-116, MCF-7, and A431) with IC₅₀s of 13.02 μM, 10.14 μM, 12.68 μM, and 47.05 μM, respectively .

HY-163371

EGFR WT/T790M-IN-1	EGFR Apoptosis	Cancer
EGFR WT/T790M-IN-1 (Compound 16h) is a dual *EGFR WT* and EGFR T790 inhibitor. EGFR WT/T790M-IN-1 can arrest the cell cycle in G2/M phase and induce apoptosis. EGFR WT/T790M-IN-1 has anti-cancer activity .

HY-162062

EGFR WT/T790M/L858R-IN-1	EGFR	Cancer
EGFR WT/T790M/L858R-IN-1 (compound 10d) is a potent *EGFR* inhibitor, with IC₅₀s of 0.097, 0.280, and 0.051?μM for *EGFR ^WT, EGFR* ^T790M, and EGFR ^L858R, respectively. EGFR WT/T790M/L858R-IN-1 can be used for the research of cancer .

HY-157994

EGFR WT/T790M-IN-2	EGFR Apoptosis	Cancer
EGFR WT/T790M-IN-2 (Compound 7c) is a EGFR T790M/WT inhibitor with IC₅₀ values of 0.08 and 0.13 μM, respectively. EGFR WT/T790M-IN-2 induces apoptosis by blocking the G0-G1 phase (apoptosis). EGFR WT/T790M-IN-2 has antitumor activity .

HY-156741

EGFR-IN-87	EGFR	Cancer
EGFR-IN-87 is a *EGFR* tyrosine kinase inhibitor. EGFR-IN-87 has IC₅₀ value of 3.1 nM, 1.3 nM and 7.1 nM for EGFR_d746-750, EGFR_L858R/T790 and EGFR_WT in A431 cells, respectively. EGFR-IN-87 can be used for cancer diseases research .

HY-152144

EGFR-IN-75	EGFR	Cancer
EGFR-IN-75 is an *EGFR ^WT* and EGFR ^T790M inhibitor with IC₅₀ values of 0.28 μM and 5.02 μM, respectively. EGFR-IN-75 shows anticancer and antioxidant activity .

HY-158149

T-1-PMPA	EGFR Apoptosis	Cancer
T-1-PMPA is a potent *EGFR* inhibitor with apoptotic properties. T-1-PMPA effectively inhibits EGFR ^WT and EGFR ^790m, with IC₅₀ values of 86 nM and 561.73 nM, respectively .

HY-141640

MS154	PROTACs EGFR	Cancer
MS154 is a first-in-class E3 ligase cereblon-recruiting *EGFR* degrader with K_ds of 1.8 nM and 3.8 nM for EGFR ^WT and EGFR ^L858R mutants. MS154 potently inhibits cell proliferation in lung cancer cells .

HY-19815

Olafertinib	EGFR	Cancer
Olafertinib is a third-generation *EGFR* TKI, with GI₅₀ values of 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19) and 689 nM (EGFR* WT*), respectively. Olafertinib has the potential for NSCLC research .

HY-161045

T-1-DOCA	EGFR Apoptosis	Cancer
T-1-DOCA ia a *EGFR* inhibitor, with the IC₅₀ of 56.94 and 269.01?nM for EGFR ^WT and EGFR ^T790M, respectively. T-1-DOCA can induces cell apoptosis of HCT-116 cells .

HY-138751A

limertinib diTFA ASK120067 diTFA	EGFR	Cancer
limertinib (ASK120067) diTFA is a potent and orally active inhibitor of EGFR ^T790M (IC₅₀: 0.3 nM) with selectivity over *EGFR* ^WT (IC₅₀: 6.0 nM). limertinib diTFA is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC) .

HY-147826

EGFR-IN-60	EGFR Apoptosis	Cancer
EGFR-IN-60 (Compound 7d) shows obvious inhibition of *EGFR ^WT, EGFR* ^T790M, EGFR ^L858R and JAK3 with IC₅₀s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR ^T790M mutation (IC₅₀=1.32 µM) over A431 cells overexpressing EGFR ^WT (IC₅₀=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio .

HY-138751

limertinib ASK120067	EGFR	Cancer
limertinib (ASK120067) is a potent and orally active inhibitor of EGFR ^T790M (IC₅₀:0.3 nM) with selectivity over EGFR ^WT (IC₅₀:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC) .

HY-143319

SPH5030	Others	Cancer
SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2 ^WT and EGFR ^WT with IC₅₀s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer .

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-128778

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

HY-150611

EGFR-IN-70	EGFR	Cancer
EGFR-IN-70 (compound 18j) is a potent *EGFR* inhibitor with IC₅₀ values of 23.6 and 307.5 nM for EGFR ^LR/TM/CS and EGFR ^WT, respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR. EGFR-IN-70 can be used for cancer research .

HY-125841

EGFR mutant-IN-1	EGFR	Cancer
EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFR ^{L858R/T790M/C797S} mutant inhibitor with an IC₅₀ of 27.5 nM, while being a significantly less potent for *EGFR ^WT* (IC₅₀ >1.0 μM) .

HY-144044

EGFR-IN-30	EGFR	Cancer
EGFR-IN-30 is a potent *EGFR* inhibitor with IC₅₀s of 1-10 nM, <1 nM for EGFR (WT), EGFR (L858R/T790M/C797S), respectively. EGFR-IN-30 has potential for cell proliferative diseases, such as cancer research .

HY-144760

EGFR-IN-3	EGFR Apoptosis	Cancer
EGFR-IN-3 (Compound 4c) is a potent *EGFR* inhibitor with an IC₅₀ of 0.32 µM against *EGFRwt-TK. EGFR-IN-3 shows cytotoxic activity against cancer cell lines and induces apoptosis* .

HY-147942

MS9449	PROTACs EGFR	Cancer
MS9449 is a potent PROTAC EGFR degrader with K_ds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer .

HY-162360

EGFR-IN-109	Apoptosis EGFR Caspase Bcl-2 Family	Cancer
EGFR-IN-109 (compound 4) is an EGFR inhibitor, with the IC₅₀ values of 25.8 and 182.3 nM for EGFR ^WT and EGFR ^T790M, respectively. EGFR-IN-109 arrests the cancer cells’ growth at the G2/M phase and induces both early and late apoptosis. EGFR-IN-109 can be used in cancer research .

HY-144053

EGFR-IN-36	EGFR	Cancer
EGFR-IN-36 is a potent *EGFR* inhibitor with IC₅₀s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research .

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-147941

MS9427	PROTACs EGFR	Cancer
MS9427 is a potent PROTAC EGFR degrader with K_ds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer .

HY-18750A

Zorifertinib hydrochloride AZD3759 hydrochloride	EGFR Apoptosis	Cancer
Zorifertinib (AZD3759) hydrochloride is a potent, orally active, central nervous system-penetrant, *EGFR* inhibitor (IC₅₀s: 0.3, 0.2, and 0.2 nM for EGFR ^wt, EGFR ^L858R, and EGFR ^{exon 19Del}, respectively). Zorifertinib hydrochloride induces cancer cell apoptosis. Zorifertinib hydrochloride has antitumor activity, and can be used for NSCLC, HCC etc. research .

HY-18750

Zorifertinib 5 Publications Verification AZD3759	EGFR Apoptosis	Cancer
Zorifertinib (AZD3759) is a potent, orally active, central nervous system-penetrant, *EGFR* inhibitor. At K_m ATP concentrations, the IC₅₀s are 0.3, 0.2, and 0.2 nM for EGFR ^wt, EGFR ^L858R, and EGFR ^{exon 19Del}, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research .

HY-128862

EGFR-IN-7	EGFR	Cancer
EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC₅₀ values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers .

HY-15729

Rociletinib 10+ Cited Publications CO-1686; AVL-301; CNX-419	EGFR	Cancer
Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of *EGFR* including T790M, and the K_i values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

HY-147941A

MS9427 TFA	PROTACs EGFR	Cancer
MS9427 TFA is a potent PROTAC EGFR degrader with K_ds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer .

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 .

HY-15729A

Rociletinib hydrobromide 10+ Cited Publications CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide	EGFR	Cancer
Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of *EGFR* including T790M, and the K_i values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

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-10261S1

Afatinib-d4 BIBW 2992-d₄	EGFR Autophagy	Cancer
Afatinib-d₄ is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.

HY-101450

PF-6274484
PF-6274484 is a potent *EGFR* inhibitor with K_is of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC₅₀s of 6.6 and 5.8 nM, respectively .

HY-132842

Sunvozertinib 1 Publications Verification DZD9008	EGFR Btk	Cancer
Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC₅₀s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52) .

HY-10261AS

Afatinib-d6 dimaleate BIBW 2992MA2-d₆	Isotope-Labeled Compounds EGFR Autophagy	Cancer
Afatinib-d₆ (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively[1][2].

HY-10261

Afatinib Maximum Cited Publications 54 Publications Verification 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-10261A

Afatinib dimaleate Maximum Cited Publications 54 Publications Verification 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-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-119944

JND3229	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-10261E

(R)-Afatinib (R)-BIBW 2992	EGFR c-Met/HGFR p38 MAPK	Cancer
(R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) 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-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-129550

BI-4020	EGFR	Cancer
BI-4020 is a fourth-generation, orally active, and non-covalent *EGFR* tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC₅₀=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC₅₀=1 nM). BI-4020 also shows activity against EGFR wt (IC₅₀=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties .

HY-143445

EGFR-IN-48	EGFR	Cancer
EGFR-IN-48 is a potent and orally active *EGFR* inhibitor with IC₅₀s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR ^d19/TM/CS, EGFR ^LR/TM/CS, EGFR ^WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3 ^{EGFR del19/T790M/C797S} and PC-9 ^{EGFR del19/T790M/C797S} cells with IC₅₀s of 1.526, 66.7 nM, respectively .

HY-149401

EGFR-IN-82	EGFR	Cancer
EGFR-IN-82 (Cmpound 8a) is a potent and orally active *EGFR* inhibitor with IC₅₀ values of 0.09 and 0.06 nM for EGFR ^{L858R/T790M/C797S} and EGFR ^{Del19/T790M/C797S}, respectively. EGFR-IN-82 has no significant effect on EGFR ^WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .

HY-139920

Oritinib 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-155736

MAPK-IN-2	p38 MAPK EGFR Raf CDK c-Met/HGFR	Cancer
MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFR ^WT IC₅₀=281 nM, c-MET IC₅₀=205 nM, B-RAF ^WT IC₅₀=112 nM, and CDK4/6 IC₅₀=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFR ^T790M IC₅₀=69 nM and B-RAF ^V600E IC₅₀=83 nM) .

HY-155178

Antiproliferative agent-34	EGFR	Cancer
Antiproliferative agent-34 (Compound A14) is a multi-target kinase inhibitor, with an IC₅₀ of 177 nM and 1567 nM for EGFR L858R/T790M and *EGFR WT. Antiproliferative agent-34 also inhibits JAK2, ROS1, FLT3, FLT4, PDGFRα with IC₅₀* of 30.93, 106.90, 108.00, 226.60, 42.53 nM. Antiproliferative agent-34 inhibits H1975 and HCC827 cells proliferation with IC₅₀ values below 40 nM under normoxic condition, and the anti-proliferation potency achieves 4–6-fold improvement (IC₅₀ values < 10 nM) under hypoxic condition .

HY-149824

EGFR T790M/L858R-IN-2	EGFR Apoptosis	Cancer
EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC₅₀ values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity .

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