Search Result

Results for "

mutant EGFR kinase

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (61) ADC Antibody (1) Akt (6) Anaplastic lymphoma kinase (ALK) (2) Apoptosis (12) Bcl-2 Family (1) BMX Kinase (1) Btk (1) c-Kit (1) Cannabinoid Receptor (1) Caspase (2) Drug Intermediate (1) Endogenous Metabolite (1) ERK (7) FAK (2) Ferroptosis (1) Glutathione Peroxidase (1) JAK (2) MEK (1) mTOR (2) p38 MAPK (1) PROTACs (2) Reactive Oxygen Species (ROS) (1) Reference Standards (4) STAT (1) TRP Channel (3)
By Research Areas:	Cancer (63) Infection (1) Inflammation/Immunology (3) Metabolic Disease (1) Neurological Disease (1)
Click Chemistry:	Alkynes (2)

Inhibitors & Agonists

Biochemical Assay Reagents

Inhibitory Antibodies

Click Chemistry

Targets Recommended: EGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-109061

Lazertinib 3 Publications Verification YH25448; GNS-1480	Apoptosis Akt TRP Channel EGFR ERK	Infection Neurological Disease Metabolic Disease Cancer
Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation *EGFR* tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of *EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC* activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .

HY-15729

Rociletinib Maximum Cited Publications 14 Publications Verification 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-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-126077

MTI-31 1 Publications Verification LXI-15029	mTOR	Inflammation/Immunology Cancer
MTI-31 (LXI-15029) is a potent, orally active and highly selective inhibitor of mTORC1 and mTORC2. MTI-31 is selective for mTOR (K_d: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity in mTOR binding assays. MTI-31 shows an IC₅₀ of 39 nM for mTOR in LANCE assay of mTOR substrate phosphorylation with 100 μM ATP. MTI-31 can be used for the research of breast cancer .

HY-13464

ALK-IN-1 Brigatinib analog	Anaplastic lymphoma kinase (ALK) EGFR	Cancer
ALK-IN-1 is an orally active, blood-brain barrier-permeable ALK and *EGFR* inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer .

HY-59219

Cyclopropylboronic acid	Drug Intermediate	Cancer
Cyclopropylboronic acid is an intermediate. Cyclopropylboronic acid can be used to synthesize *EGFR* kinase inhibitor (Compound 25). Compound 25 has antiproliferative effects on EGFR mutant (EGFR Δ19del/T790M/C797S) cells. Cyclopropylboronic acid can be used in lung cancer research .

HY-109061B

Lazertinib mesylate 3 Publications Verification YH25448 mesylate; GNS-1480 mesylate	TRP Channel EGFR Akt ERK Apoptosis	Cancer
Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation *EGFR* tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of *EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC* activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .

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-157229

STX-721 1 Publications Verification	EGFR ERK	Cancer
STX-721 is an orally active, irreversible, covalent *EGFR* exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of *EGFR* (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .

HY-12972

Mavelertinib PF-06747775	EGFR	Cancer
Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC₅₀s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC) .

HY-134877

BAY 2476568	EGFR ERK Akt	Cancer
BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC₅₀ values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits *EGFR* (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations .

HY-104066

Theliatinib Xiliertinib; HMPL-309	EGFR	Cancer
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective *EGFR* inhibitor with a K_i of 0.05 nM and an IC₅₀ of 3 nM. Theliatinib has an IC₅₀ of 22 nM for **EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR** than other kinases . Theliatinib 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-17499

EGFR-IN-12	EGFR Apoptosis	Cancer
EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective *EGFR* inhibitor with an IC₅₀of 21 nM. EGFR-IN-12 also inhibits mutant EGFR ^L858R and EGFR ^L861Q with IC₅₀s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for *EGFR* over HER4 (IC₅₀ = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity .

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-15729A

Rociletinib hydrobromide Maximum Cited Publications 14 Publications Verification 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-161633

PROTAC EGFR degrader 11	PROTACs EGFR FAK	Cancer
PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC₅₀ <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a K_i of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC₅₀ <100 nM.

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-P990947

Tilatamig AZD9592 Antibody	ADC Antibody EGFR	Cancer
Tilatamig (AZD9592 Antibody) is a human antibody of the Ig (G1-κ_G1-λ2) subtype that targets *EGFR/MET. Tilatamig conjugates with the Top1* inhibitor AZ14170133 (HY-145399) to form the antibody-drug conjugate (ADC) Tilatamig samrotecan (HY-171124) (AZD9592). Tilatamig accurately targets NSCLC models including EGFR-mutant, EGFR-wildtype, and EGFR tyrosine kinase inhibitor-treated ones, and its activity correlates with high expression of *EGFR, c-MET* and SLFN11. Tilatamig is available for in vivo anti-tumor studies in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) .

HY-17654

BIEGi-1	EGFR mTOR	Cancer
BIEGi-1 is an *EGFR* inhibitor. BIEGi-1 effectively disrupts the *EGFR-Rheb* interaction in cells. BIEGi-1 robustly inhibits *EGFR* kinase activity (reduces p-Y1068-EGFR) as well as mTORC1 activation (reduces p-T389-S6K1) in EGFR-mutant cells. BIEGi-1 shows strong antiproliferative effects on EGFR-mutant PC9 and HCC827 cells with IC₅₀ values of 17 nM and 20 nM, respectively. BIEGi-1 can be used for the study of cancers harboring EGFR mutations, such as non-small cell lung cancer (NSCLC) .

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-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-130616

EGFR-IN-11	EGFR Apoptosis	Cancer
EGFR-IN-11 is a fourth-generation *EGFR*-tyrosine kinase inhibitor (EGFR-TKI) with an IC₅₀ of 18 nM for triple mutant EGFR ^{L858R/T790M/C797S}. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1 .

HY-174826

EGFR-IN-164	EGFR c-Kit	Cancer
EGFR-IN-164 (Compound 4) is a selective and covalent allosteric *EGFR* inhibitor. EGFR-IN-164 significantly inhibits the activity of EGFR ^{L858R/T790M/C797S} kinase (IC₅₀: 48.1 nM) and proliferation of of EGFR-mutant cells. EGFR-IN-164 can be used for drug resistance of cancer research .

HY-161632

PROTAC EGFR degrader 10	PROTACs EGFR FAK	Cancer
PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC₅₀ <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a K_i of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC₅₀ <150 nM .

HY-W740378

1,2,3,4-Tetrahydro Staurosporin AFN-941	EGFR JAK	Others
1,2,3,4-Tetrahydrostaurosporine is a derivative of Staurosporine (HY-15141) and an inhibitor of mutant EGFR (IC₅₀=74 nM for EGFRT790M). It is selective for EGFRT790M over wild-type EGFR (IC₅₀=390 nM). It also binds to Janus kinase 3 (JAK3).

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-17499R

EGFR-IN-12 (Standard)	EGFR Apoptosis	Cancer
EGFR-IN-12 (Standard) is the analytical standard of EGFR-IN-12. This product is intended for research and analytical applications. EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFRL858R and EGFRL861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity .

HY-178448

EGFR-IN-178	EGFR JAK Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Cannabinoid Receptor Glutathione Peroxidase Caspase	Inflammation/Immunology Cancer
EGFR-IN-178 is an orally active *EGFR* mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the *EGFR* enzyme, including Del19 (IC₅₀ = 3.4 nM), L858R/T790 M (IC₅₀ = 2.9 nM), and Del19/T790 M (IC₅₀ = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC₅₀ = 55.6 nM) and JAK3 (IC₅₀ = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC) .

HY-E70696

EGFR C797S/L858R Recombinant Human Active Protein Kinase	EGFR	Cancer
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR C797S/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR C797S/L858R protein that can be used to study EGFR C797S/L858R-related functions .

HY-15729R

Rociletinib (Standard) CO-1686 (Standard); AVL-301 (Standard); CNX-419 (Standard)	EGFR Reference Standards	Cancer
Rociletinib (Standard) is the analytical standard of Rociletinib. This product is intended for research and analytical applications. Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

HY-15729AR

Rociletinib hydrobromide (Standard) CO-1686 hydrobromide (Standard); AVL-301 hydrobromide (Standard); CNX-419 hydrobromide (Standard)	EGFR Reference Standards	Cancer
Rociletinib hydrobromide (Standard) is the analytical standard of Rociletinib hydrobromide. This product is intended for research and analytical applications. Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

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-164056

EGFR T790M/L858R-IN-8	EGFR	Cancer
EGFR T790M/L858R-IN-8 (Compound 9) is a selective EGFR ^T790M/L858R mutant kinase inhibitor with a IC₅₀ of 56.8 μM, and it shows no inhibitory activity against wild-type *EGFR. EGFR* T790M/L858R-IN-8 can be used for the research of non-small cell lung cancer .

HY-162300

EGFR kinase inhibitor 4	EGFR	Cancer
EGFR kinase inhibitor 4 (Compound 4) is a bivalent ATP-allosteric *EGFR* inhibitor (IC₅₀: 1.8 nM for mutant EGFR (LRTMCS)). EGFR kinase inhibitor 4 can be used for research of NSCLC .

HY-18213

EGFR-IN-9	EGFR	Cancer
EGFR-IN-9 (Compound 8) is a potent **EGFR kinase inhibitor with IC₅₀*s 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-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-157166

EGFR kinase inhibitor 2	EGFR	Cancer
EGFR kinase inhibitor 2 (compound A-7) is a potent EGFR inhibitor targeting EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S mutants. EGFR kinase inhibitor 2 has the potential to address acquired resistance in the treatment of non-small cell lung cancer .

HY-172780

EGFR-IN-161	EGFR Apoptosis	Cancer
EGFR-IN-161 (Compound DD-8) is a potent and reversible inhibitor of L858R/T790M/C797S mutant EGFR kinases, with an IC₅₀ of 0.87 nM. EGFR-IN-161 can induce apoptosis process, G1-phase arrestation, and migration inhibition in tumor cells .

HY-E70704

EGFR G719C Recombinant Human Active Protein Kinase	EGFR	Cancer
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR G719C Recombinant Human Active Protein Kinase is a recombinant EGFR G719C protein that can be used to study EGFR G719C-related functions .

HY-E70695

EGFR C797S Recombinant Human Active Protein Kinase	EGFR	Cancer
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR C797S Recombinant Human Active Protein Kinase is a recombinant EGFR C797S protein that can be used to study EGFR C797S-related functions .

HY-E70707

EGFR L858R Recombinant Human Active Protein Kinase	EGFR	Cancer
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L858R Recombinant Human Active Protein Kinase is a recombinant EGFR L858R protein that can be used to study EGFR L858R-related functions .

HY-E70708

EGFR L861Q Recombinant Human Active Protein Kinase	EGFR	Cancer
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L861Q Recombinant Human Active Protein Kinase is a recombinant EGFR L861Q protein that can be used to study EGFR L861Q-related functions .

HY-E70706

EGFR L718Q Recombinant Human Active Protein Kinase	EGFR	Cancer
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR L718Q Recombinant Human Active Protein Kinase is a recombinant EGFR L718Q protein that can be used to study EGFR L718Q-related functions .

HY-E70705

EGFR G719S Recombinant Human Active Protein Kinase	EGFR	Cancer
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR G719S Recombinant Human Active Protein Kinase is a recombinant EGFR G719S protein that can be used to study EGFR G719S-related functions .

HY-E70697

EGFR d746-750 Recombinant Human Active Protein Kinase	EGFR	Cancer
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750 Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750 protein that can be used to study EGFR d746-750-related functions .

HY-E70703

EGFR d752-759 Recombinant Human Active Protein Kinase	EGFR	Cancer
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d752-759 Recombinant Human Active Protein Kinase is a recombinant EGFR d752-759 protein that can be used to study EGFR d752-759-related functions .

HY-13464R

ALK-IN-1 (Standard) Brigatinib analog (Standard)	Reference Standards Anaplastic lymphoma kinase (ALK) EGFR	Cancer
ALK-IN-1 (Standard) is the analytical standard of ALK-IN-1 (Brigatinib analog) (HY-13464). This product is intended for research and analytical applications. ALK-IN-1 is an ALK and *EGFR* inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer .

HY-E70709

EGFR T790M Recombinant Human Active Protein Kinase	EGFR	Cancer
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR T790M Recombinant Human Active Protein Kinase is a recombinant EEGFR T790M protein that can be used to study EGFR T790M-related functions .

HY-164464

BPI-15086	EGFR	Cancer
BPI-15086 an orally active, potent, irreversible mutant-selective inhibitor of both *EGFR* and T790M resistance mutations tyrosine kinase. BPI-15086 can be used for the research of non-small-cell lung cancer .

Cat. No.	Product Name	Target	Research Area	Image

HY-P990947

Tilatamig AZD9592 Antibody	ADC Antibody EGFR	Cancer
Tilatamig (AZD9592 Antibody) is a human antibody of the Ig (G1-κ_G1-λ2) subtype that targets *EGFR/MET. Tilatamig conjugates with the Top1* inhibitor AZ14170133 (HY-145399) to form the antibody-drug conjugate (ADC) Tilatamig samrotecan (HY-171124) (AZD9592). Tilatamig accurately targets NSCLC models including EGFR-mutant, EGFR-wildtype, and EGFR tyrosine kinase inhibitor-treated ones, and its activity correlates with high expression of *EGFR, c-MET* and SLFN11. Tilatamig is available for in vivo anti-tumor studies in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) .

Cat. No.	Product Name		Classification

HY-104066

Theliatinib Xiliertinib; HMPL-309		Alkynes
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective *EGFR* inhibitor with a K_i of 0.05 nM and an IC₅₀ of 3 nM. Theliatinib has an IC₅₀ of 22 nM for **EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR** than other kinases . Theliatinib 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-104066A

Theliatinib tartrate Xiliertinib tartrate; HMPL-309 tartrate		Alkynes
Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective *EGFR* inhibitor with a K_i of 0.05 nM and an IC₅₀ of 3 nM. Theliatinib has an IC₅₀ of 22 nM for **EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR** than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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