Search Result

Isoforms Recommended:	EGFR/ErbB1/HER1

Results for "

EGFR WT

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (79) Akt (6) Anaplastic lymphoma kinase (ALK) (1) Apoptosis (25) Autophagy (4) Bcl-2 Family (2) BMX Kinase (1) Btk (2) c-Met/HGFR (6) Caspase (2) CDK (1) COX (1) Cytochrome P450 (1) Drug Derivative (1) ERK (3) JNK (1) MEK (1) Microtubule/Tubulin (1) mTOR (1) p38 MAPK (6) PERK (1) PI3K (1) Pim (1) Potassium Channel (1) PROTACs (6) Raf (3) Ras (1) Src (1) STAT (1) Topoisomerase (1) VEGFR (3)
By Research Areas:	Cancer (80) Infection (2) Inflammation/Immunology (5) Metabolic Disease (1) Neurological Disease (1)

Targets Recommended: EGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10261

Afatinib Maximum Cited Publications 103 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-132842

Sunvozertinib 4 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-10261A

Afatinib dimaleate Maximum Cited Publications 103 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-18750

Zorifertinib 5+ Cited Publications AZD3759	EGFR Apoptosis	Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Zorifertinib (AZD3759) is a potent, orally active, BBB-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-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-141640

MS154	PROTACs EGFR	Cancer
MS154 is a first-in-class E3 ligase cereblon-recruited *EGFR* degrader with K_d values of 1.8 nM and 3.8 nM for EGFR ^WT and EGFR ^L858R mutant, respectively. MS154 potently induces degradation of mutant, but not wild-type, EGFR in cancer cell lines in an E3 ligase-dependent manner. MS154 exhibits anticancer effects against lung cancer (blue: E3 ligase ligand (HY-103596); black: linker (HY-W096167); pink: EGFR ligand (HY-168305)) .

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-138751

limertinib 1 Publications Verification 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-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-13984

NT-1 1 Publications Verification EGFR mutant-IN-3	EGFR ERK Apoptosis Drug Derivative	Cancer
NT-1 (EGFR mutant-IN-3) is a potent mutant *EGFR* inhibitor and an analog of Osimertinib (HY-15772). This mutant EGFR inhibitor suppresses FGFR ^WT with an IC₅₀ of 0.4 nM. NT-1 also inhibits EGFR ^L858R, EGFR ^{Exon 19 deletion} and EGFR ^T790M. NT-1 exerts deeper inhibition on *p-EGFR* and p-ERK, and induces tumor cell apoptosis. NT-1 can be used in colorectal cancer research .

HY-111138

CZC-8004 CZC-00008004	EGFR VEGFR	Cancer
CZC-8004 (CZC-00008004) is a pan-kinase inhibitor. CZC-8004 has IC₅₀ values of 650 and 437 nM for EGFR WT and VEGFR2 V916M, respectively. CZC-8004 can be used in the study of 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-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-163428

Perzebertinib ZN-A-1041	EGFR	Inflammation/Immunology Cancer
ZN-A-1041 inhibits HER2 in BT474 cell and *wt-EGFR* in H838 cells, with IC₅₀s of 9.5 nM and 12 μM respectively. ZN-A-1041 can be used for research of cancer and inflammation .

HY-175252

*PROTAC EGFR* degrader 14**	PROTACs EGFR Apoptosis	Cancer
PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC₅₀ of about 2.9 nM and a D_max of 93.1% for EGFR ^{L858R/T790M/C797S}. PROTAC EGFR degrader 14 selectively induces EGFR ^C797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFR ^WT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688)) .

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-147941

MS9427	PROTACs EGFR	Inflammation/Immunology 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-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-143319

SPH5030	EGFR	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-101450

PF-6274484	EGFR	Cancer
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-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-138751A

limertinib diTFA 1 Publications Verification 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-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-147941A

MS9427 TFA	PROTACs EGFR	Infection Inflammation/Immunology 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-156741A

EGFR-IN-87 hydrochloride	EGFR	Cancer
EGFR-IN-87 (Compound Example 2) hydrochloride is a *EGFR* tyrosine kinase inhibitor. EGFR-IN-87 hydrochloride 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 hydrochloride can be used for cancer diseases research .

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-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-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-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-156741

EGFR-IN-87	EGFR	Cancer
EGFR-IN-87 (Compound Example 2) 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-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-178442

EGFR-IN-179	EGFR	Cancer
EGFR-IN-179 (Compound 8d) is an *EGFR* inhibitor (IC₅₀: 0.068 μM for EGFR L858R/T790M/C797S; 2.56 μM for EGFR-WT-TK). EGFR-IN-179 has anticancer activity against non-small cell lung cancer .

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-18750A

Zorifertinib hydrochloride AZD3759 hydrochloride	EGFR Apoptosis	Cancer
Zorifertinib (AZD3759) hydrochloride is a potent, orally active, BBB-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-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-175292

EGFR WT/T790M-IN-3	EGFR Microtubule/Tubulin	Cancer
EGFR WT/T790M-IN-3 is an irreversible covalent EGFR ^WT and EGFR ^T790M inhibitor with IC₅₀s value of 28.1 and 24.6 nM. EGFR WT/T790M-IN-3 hampers tubulin polymerization through IC₅₀ value of 5.1 μM. EGFR WT/T790M-IN-3 shows significant anti-proliferative effects on HCT116 and T47D cells, with IC₅₀ values of 3.12 and 4.12 μM, respectively. EGFR WT/T790M-IN-3 can be used for the study of cancers such as non-small cell lung cancer, colon cancer and breast 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-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-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-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-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-W1126467

RAS-IN-5	Ras	Cancer
RAS-IN-5 (Example 2) is a RAS inhibitor. RAS-IN-5 significantly inhibits the interaction between RAF1 and active KRAS mutant protein or HRAS WT protein. RAS-IN-5 significantly inhibits the cell viability of KRAS, NRAS, and EGFR mutant cells. RAS-IN-5 can be used in the research of colorectal cancer, liver cancer, and non-small cell lung cancer .

HY-179098

Multi-target kinase-IN-8	Raf c-Met/HGFR Pim EGFR VEGFR Apoptosis	Cancer
Multi-target kinase-IN-8 (3d) is an anti-cancer agent. Multi-target kinase-IN-8 exhibits inhibitory activity against various protein kinases (B-Raf V600E (IC₅₀ = 0.078 µg/mL), c-Met (IC₅₀ = 0.405 µg/mL), Pim-1 (IC₅₀ = 1.053 µg/mL), EGFR WT (IC₅₀ = 0.177 µg/mL), VEGFR-2 (IC₅₀ = 0.275 µg/mL)). Multi-target kinase-IN-8 can induce cell cycle arrest and promote early and late apoptosis. Multi-target kinase-IN-8 is commonly 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-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-162623

EGFR/HER2-IN-15	EGFR	Cancer
EGFR/HER2-IN-15, a dihydropyrimidine, is a potent *EGFR/HER2* inhibitor. EGFR/HER2-IN-15 significantly inhibits EGFR ^wt activity with an IC₅₀ of 37.21 nM. EGFR/HER2-IN-15 has anticaner effects .

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-169982

EGFR-IN-136	EGFR	Cancer
EGFR-IN-136 (compound 21v) is a potent *EGFR* inhibitor with IC₅₀ values of 20.2, 1.2, 2.3, 12.5 nM for EGFR ^WT, EGFR ^LR/TM, EGFR ^19D/TM/CS, EGFR ^LR/TM/CS, respectively. EGFR-IN-136 shows antiproliferative activity. EGFR-IN-136 shows antitumor activity and has the potential for the research of NSCLC .

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EGFR WT

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