Search Result

Results for "

mutant EGFR

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (169) ADC Antibody (1) Akt (15) AMPK (1) Anaplastic lymphoma kinase (ALK) (7) Antibody-Drug Conjugates (ADCs) (1) Apoptosis (26) Autophagy (2) Bcl-2 Family (2) BCRP (1) Biochemical Assay Reagents (2) BMX Kinase (1) Btk (3) c-Kit (1) Cannabinoid Receptor (1) Caspase (3) CDK (1) COX (1) Cytochrome P450 (1) Discoidin Domain Receptor (1) Drug Derivative (2) Drug Intermediate (2) Endogenous Metabolite (1) ERK (13) Estrogen Receptor/ERR (1) FABP (1) FAK (3) Ferroptosis (1) Folate Receptor (FR) (5) GLUT (1) Glutathione Peroxidase (1) GSK-3 (1) Hippo (MST) (1) HSP (1) IAP (1) Interleukin Related (1) Isotope-Labeled Compounds (2) JAK (2) JNK (1) MDM-2/p53 (1) MEK (1) mTOR (3) NEKs (1) NF-κB (1) NO Synthase (1) p38 MAPK (2) PARP (1) PD-1/PD-L1 (1) PERK (2) Phosphatase (1) PI3K (3) PROTACs (18) Ras (1) Reactive Oxygen Species (ROS) (2) Reference Standards (11) ROS Kinase (1) SHP2 (1) SOD (1) SOS1 (1) STAT (2) TAM Receptor (1) Trk Receptor (1) TRP Channel (3) VEGFR (3) YAP (1)
By Research Areas:	Cancer (180) Infection (4) Inflammation/Immunology (8) Metabolic Disease (3) Neurological Disease (3)
Click Chemistry:	DBCO (5) PROTAC Synthesis (1) Alkynes (4)

188

Inhibitors & Agonists

Fluorescent Dyes

Biochemical Assay Reagents

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Antibodies

Click Chemistry

Targets Recommended: EGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-112870

Firmonertinib 5+ Cited Publications Alflutinib; Furmonertinib; AST2818	EGFR	Cancer
Firmonertinib (Alflutinib; Furmonertinib) is an orally active, mutant-selective, and highly brain penetrant *EGFR* inhibitor. Firmonertinib inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .

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-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-P99849

Depatuxizumab ABT-806	EGFR	Cancer
Depatuxizumab is a brain-penetrant and humanized tumor-specific anti *EGFR* monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .

HY-112870A

Firmonertinib mesylate 5+ Cited Publications Alflutinib mesylate; Furmonertinib mesylate; AST2818 mesylate	EGFR	Inflammation/Immunology Cancer
Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant *EGFR* inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .

HY-136789

Tuxobertinib 1 Publications Verification BDTX-189	EGFR	Cancer
Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric *EGFR* and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows K_Ds of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity .

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-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-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-19729

Naquotinib 5 Publications Verification ASP8273	EGFR	Cancer
Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible *EGFR* inhibitor; with IC₅₀s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

HY-12872

Nazartinib 5+ Cited Publications EGF816	EGFR	Cancer
Nazartinib (EGF816) is a covalent mutant-selective *EGFR* inhibitor, with K_i and K_inact of 31 nM and 0.222 min ⁻¹ on EGFR(L858R/790M) mutant, respectively.

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-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-19985

PF-06459988	EGFR	Cancer
PF-06459988 is an orally activity, irreversible and mutant-selective inhibitor of *EGFR* mutant forms. PF-06459988 demonstrates high potency and specificity to the T790M-containing double mutant EGFRs. PF-06459988 can be used for the research of cancer .

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-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-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-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-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-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-19803

Naquotinib mesylate 5 Publications Verification ASP8273 mesylate	EGFR	Cancer
Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible *EGFR* inhibitor; with IC₅₀s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

HY-13897

CNX-2006	EGFR	Cancer
CNX-2006 is a mutant-selective and irreversible *EGFR* inhibitor with an IC₅₀ below 20 nM for EGFR ^T790M.

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-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-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-153974

BBT-176	EGFR	Cancer
BBT-176 is an orally effective *EGFR* inhibitor. BBT-176 has inhibitory activity against multiple EGFR C797S mutant cell lines. BBT-176 is commonly used in cancer research .

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-15801

HG-14-10-04	Anaplastic lymphoma kinase (ALK) EGFR	Cancer
HG-14-10-04 is a potent ALK and mutant *EGFR* inhibitor with IC₅₀s of 20 nM, 15.6 nM, 22.6 nM and 124.5 nM for ALK, EGFR ^LR/TM, EGFR ^19del/TM/CS and EGFR ^LR/TM/CS, respectively. HG-14-10-04 can be used to research 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-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-W002798

Cyclopropanesulfonyl chloride	Biochemical Assay Reagents Drug Intermediate	Cancer
Cyclopropanesulfonyl chloride is an intermediate. Cyclopropanesulfonyl chloride can be used to synthesize Compound 1. Compound 1 has anticancer activity against EGFR triple-mutant tumors .

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-155537

Pruvonertinib 1 Publications Verification YK-029A	EGFR	Cancer
YK-029A is an orally active inhibitor of mutant *EGFR*，targeting to both the T790M mutations (EGFR ^T790M) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity，and results tumor regression in EGFRex20ins-driven PDX models .

HY-W423595

BEBT-109	EGFR	Cancer
BEBT-109 is a potent pan-mutant-selective *EGFR* inhibitor. BEBT-109 has improved pharmacokinetic properties. BEBT-109 can be used for multiple mutant-EGFR-driven non-small cell lung cancer (NSCLC) research .

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-176556

EGFR-IN-167	EGFR	Cancer
EGFR-IN-1671 is a selective *EGFR* inhibitor with an IC₅₀ of 0.19 nM. EGFR-IN-167 exhibits good potency against various EGFR mutants (IC₅₀ = 0.109 nM, 0.75 nM and <0.05 nM against EGFR (L858R), EGFR (C797S) and EGFR (del19), respectively). EGFR-IN-1671 covalently engages the catalytically conserved lysine of EGFR in live mammalian cells. EGFR-IN-1671 demonstrates excellent anti-proliferative activity by inhibiting EGFR autophosphorylation. EGFR-IN-1671 can be used for the study of non-small-cell lung carcinomas (NSCLC), glioblastoma and many solid tumors .

HY-131067

EMI56	EGFR	Cancer
EMI56, the derivative of EMI1, displays greater potency toward mutant *EGFR* than EMI1. EMI56 inhibits *EGFR* triple mutants .

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 IC₅₀*s 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-144605

PROTAC EGFR degrader 3	EGFR PROTACs	Cancer
PROTAC EGFR degrader 3 is a potent PROTAC *EGFR* degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation .

HY-123766

EGFR-IN-99	EGFR	Cancer
EGFR-IN-99 (compound 1a) is a potent *EGFR* and HER2 Exon 20 insertion mutant inhibitor. EGFR-IN-99 has excellent antiproliferative activity against DFCI127 cells, with an EC₅₀ of 11.5 nM. EGFR-IN-99 can be used for the research of non-small cell lung cancer (NSCLC) .

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-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-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-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-155005

EGFR mutant-IN-2	EGFR	Cancer
EGFR mutant-IN-2 (Compound D51) is an *EGFR* mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFR ^{L858R/T790M/C797S} mutant with an IC₅₀ value of 14 nM. EGFR mutant-IN-2 inhibits the EGFR ^{del19/T790M/C797S} mutant with an IC₅₀ value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity .

Cat. No.	Product Name	Type

HY-59219

Cyclopropylboronic acid	Biochemical Assay Reagents
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-W1123936B

DBCO-PEG1000-FA

DBCO-PEG1000-Folate

Biochemical Assay Reagents

DBCO-PEG1000-FA (DBCO-PEG1000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .

HY-W002798

Cyclopropanesulfonyl chloride	Biochemical Assay Reagents
Cyclopropanesulfonyl chloride is an intermediate. Cyclopropanesulfonyl chloride can be used to synthesize Compound 1. Compound 1 has anticancer activity against EGFR triple-mutant tumors .

HY-W1123936C

DBCO-PEG2000-FA

DBCO-PEG2000-Folate

Biochemical Assay Reagents

DBCO-PEG2000-FA (DBCO-PEG2000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .

HY-W1123936D

DBCO-PEG3400-FA

DBCO-PEG3400-Folate

Biochemical Assay Reagents

DBCO-PEG-FA (DBCO-PEG-Folate) (MW 3400) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .

HY-W1123936H

DBCO-PEG10000-FA

DBCO-PEG10000-Folate

Biochemical Assay Reagents

DBCO-PEG10000-FA (DBCO-PEG10000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .

HY-W1123936E

DBCO-PEG5000-FA

DBCO-PEG5000-Folate

Biochemical Assay Reagents

DBCO-PEG5000-FA (DBCO-PEG5000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .

HY-W1123937C

Biotin-PEG5000-CHO	Biochemical Assay Reagents
Biotin-PEG-CHO (with a molecular weight of 5000) is a biotin-attached PEG derivative that can be used for biotinylation of biological molecules or other material surfaces. Biotin can be easily detected through the biotin/streptavidin binding test, and is widely used in molecular targeted detection.

Cat. No.	Product Name	Target	Research Area	Image

HY-P99849

Depatuxizumab ABT-806	EGFR	Cancer
Depatuxizumab is a brain-penetrant and humanized tumor-specific anti *EGFR* monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on 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-P991571

GC1118 GC-1118A	EGFR PERK Akt	Cancer
GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (K_D) to *EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR* ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2445

Flavokawain C 4 Publications Verification	Structural Classification Classification of Application Fields Piperaceae Plants Chalcones Flavonoids other families Phenols Polyphenols Piper methysticum G.Forst. Disease Research Fields Source Classification Cancer	Apoptosis Akt JNK PERK Caspase PARP MDM-2/p53 IAP Reactive Oxygen Species (ROS) SOD FABP Autophagy AMPK mTOR GLUT EGFR PI3K HSP VEGFR FAK
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the *EGFR/PI3K/Akt/mTOR* signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .

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.

HY-112870AS

Firmonertinib-d3 mesylate

Firmonertinib-d₃ (Alflutinib-d₃) mesylate is the deuterium labeled Firmonertinib mesylate (HY-112870A). Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation.

Host:	Mouse (2)
Reactivity:	Human (2)
Application:	IHC-P (2) WB (2) FC (2) ELISA (2)
Isotype:	IgG1 (2)
Conjugation:	Non-conjugated (2)
Clonality:	Monoclonal (1)
Modification:	Unmodified (1)

Cat. No.	Compare	Product Name	Application	Reactivity	Image

HY-P83891

	EGFR mutant (L858R) Antibody (YA3588) ERBB; HER1; mENA; ERBB1; PIG61; L858R mutant	WB, IHC-P, FC, ELISA	Human
	EGFR mutant (L858R) Antibody (YA3588) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to EGFR mutant.

HY-P83891A

	EGFR mutant (L858R) Antibody (YA3588)(PBS only) ERBB; HER1; mENA; ERBB1; PIG61; L858R mutant	WB, IHC-P, FC, ELISA	Human
	EGFR mutant (L858R) Antibody (YA3588) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to EGFR mutant.

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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-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-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-W1123936B

DBCO-PEG1000-FA DBCO-PEG1000-Folate		DBCO
DBCO-PEG1000-FA (DBCO-PEG1000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .

HY-W1123936C

DBCO-PEG2000-FA DBCO-PEG2000-Folate		DBCO
DBCO-PEG2000-FA (DBCO-PEG2000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .

HY-W1123936D

DBCO-PEG3400-FA DBCO-PEG3400-Folate		DBCO
DBCO-PEG-FA (DBCO-PEG-Folate) (MW 3400) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .

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.

HY-W1123936H

DBCO-PEG10000-FA DBCO-PEG10000-Folate		DBCO
DBCO-PEG10000-FA (DBCO-PEG10000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .

HY-W1123936E

DBCO-PEG5000-FA DBCO-PEG5000-Folate		DBCO
DBCO-PEG5000-FA (DBCO-PEG5000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .

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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