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EGFR-IN-1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (21) Anaplastic lymphoma kinase (ALK) (2) Apoptosis (8) Autophagy (6) c-Kit (1) Casein Kinase (1) CDK (1) Checkpoint Kinase (Chk) (1) Drug Metabolite (1) Fluorescent Dye (2) Histone Methyltransferase (1) Isotope-Labeled Compounds (3) Ligands for Target Protein for PROTAC (1) PARP (1) Pim (1) Raf (1) Target Protein Ligand-Linker Conjugates (1) Topoisomerase (1) Trk Receptor (1) VEGFR (6)
By Research Areas:	Cancer (29)
Click Chemistry:	Alkynes (2)

Inhibitors & Agonists

Inhibitory Antibodies

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: EGFR AIM2 NEKs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19617B

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

HY-78869

Mutated EGFR-IN-1 OsimertINib analog	EGFR	Cancer
Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated *EGFR, such as L858R EGFR*, Exonl9 deletion activating mutant and T790M resistance mutant.

HY-19617

*EGFR-IN-1*
EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity ^[1].

HY-19617A

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

HY-155227

ALK/EGFR-IN-1	Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
ALK/EGFR-IN-1 (Compound 8l) is an *ALK/EGFR* dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC₅₀ of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research ^[1].

HY-163434

PRMT5/EGFR-IN-1	EGFR Histone Methyltransferase	Cancer
PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual *PRMT5/EGFR* inhibitor, with IC₅₀s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors ^[1].

HY-157402

Topoisomerase II/EGFR-IN-1	Topoisomerase EGFR	Cancer
Topoisomerase II/EGFR-IN-1 is topoisomerase II/EGFR dual inhibitor. Topoisomerase II/EGFR-IN-1 has superior cytotoxic activity to MCF-7, A549 and HCT-116 cell lines, displays strong apoptotic activity and can be used for the research of cancer ^[1].

HY-100962

(E)-AG 99

(E)-TyrphostIN 46; (E)-TyrphostIN AG 99

(E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor .
HY-153744

JGK-068S

EGFR Cancer

JGK-068S (compound I) is a potent EGFR inhibitor .

(E)-AG 99 (E)-TyrphostIN 46; (E)-TyrphostIN AG 99
(E)-AG 99 ((E)-Tyrphostin 46) is a potent *EGFR* inhibitor .

JGK-068S	EGFR	Cancer
JGK-068S (compound I) is a potent *EGFR* inhibitor .

HY-141486

(Rac)-PROTAC PARP/EGFR ligand 1	Target Protein Ligand-Linker Conjugates	Cancer
(Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP ^[1].

HY-P99892

Serclutamab

PR-1594407; DC-1630423
EGFR Others

Serclutamab is a humanized chimeric antibody targeting EGFR IgG1-κ. Mainly expressed by CHO (Chinese Hamster Ovary) cells ^[1].

Serclutamab PR-1594407; DC-1630423	EGFR	Others
Serclutamab is a humanized chimeric antibody targeting EGFR IgG1-κ. Mainly expressed by CHO (Chinese Hamster Ovary) cells ^[1].

HY-18957A

rel-Lifirafenib rel-BGB-283	Others	Cancer
rel-Lifirafenib (rel-BGB-283) is the relative configuration of Lifirafenib (HY-18957). Lifirafenib is a potent Raf Kinase and EGFR inhibitor .

HY-141486A

PROTAC PARP/EGFR ligand 1	PARP EGFR Ligands for Target Protein for PROTAC	Others
PROTAC PARP/EGFR ligand 1 is an active compound that can be used for the synthesis of dual PARP EGFR degraders by proteolytic targeting chimera (PROTAC) technology ^[1].

HY-138627A

AST5902 trimesylate	EGFR Drug Metabolite	Cancer
AST5902 trimesylate is the principal metabolite of Alflutinib (AST2818) both in vitro and in vivo. AST5902 trimesylate exerts antineoplastic activity. Alflutinib is an *EGFR* inhibitor .

HY-50896S1

Erlotinib-13C6 CP-358774-¹³C₆; NSC 718781-¹³C₆; OSI-774-¹³C₆	Isotope-Labeled Compounds EGFR Autophagy	Cancer
Erlotinib- ¹³C₆ is a ¹³C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1].

HY-18957B

Lifirafenib maleate BGB-283 maleate	EGFR Raf	Others
Lifirafenib (BGB-283) maleate is a novel and potent Raf Kinase and *EGFR* inhibitor with IC₅₀ values of 23 and 29 nM for recombinant BRaf ^V600E and EGFR, respectively .

HY-135805A

(Rac)-JBJ-04-125-02

EGFR Cancer

(Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor .

(Rac)-JBJ-04-125-02	EGFR	Cancer
(Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active *EGFR* inhibitor .

HY-135805B

(Rac)-JBJ-04-125-02 acetate	EGFR	Cancer
(Rac)-JBJ-04-125-02 acetate is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, selective mutagenesis, allosteric and orally active EGFR inhibitor .

HY-21292

SU5214

SU4949

SU5214 is a potent VEGFR2 inhibitor extracted from patent US5834504A, SU5214, has IC₅₀s of 14.8 µM (FLK-1) and 36.7 µM (EGFR), respectively .

SU5214 SU4949
SU5214 is a potent VEGFR2 inhibitor extracted from patent US5834504A, SU5214, has IC₅₀s of 14.8 µM (FLK-1) and 36.7 µM (EGFR), respectively .

HY-10531

ARRY-380 analog	EGFR	Cancer
ARRY-380 analog, an inhibitor of *EGFR (ErbB1)*, is extracted from patent WO2015153959A2, compound 249 ^[1]. ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2 .

HY-D1464

CH1055 1 Publications Verification	Fluorescent Dye	Cancer
CH1055 is a NIR-II fluorophore based on a synthetic 970-Da organic molecule. CH1055 is a rapidly excreted dye (∼90% excreted through the kidneys within 24 h). CH1055 also allows targeted molecular imaging of tumors in vivo when conjugated with anti-EGFR Affibody .

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) ^[1].

HY-D1464A

CH1055 triethylamine 1 Publications Verification	Fluorescent Dye	Cancer
CH1055 triethylamine is a NIR-II fluorophore based on a synthetic 970-Da organic molecule. CH1055 triethylamine is a rapidly excreted dye (∼90% excreted through the kidneys within 24 h). CH1055 triethylamine also allows targeted molecular imaging of tumors in vivo when conjugated with anti-EGFR Affibody .

HY-10260

Vandetanib Maximum Cited Publications 18 Publications Verification ZD6474	VEGFR Autophagy Apoptosis	Cancer
Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC₅₀=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC₅₀=110 nM) and *EGFR/HER1* (IC₅₀=500 nM) ^[1].

HY-10260B

Vandetanib hydrochloride ZD6474 hydrochloride	VEGFR Autophagy Apoptosis	Cancer
Vandetanib hydrochloride (D6474 hydrochloride) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC₅₀=40 nM). Vandetanib hydrochloride also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC₅₀=110 nM) and *EGFR/HER1* (IC₅₀=500 nM) ^[1].

HY-10260A

Vandetanib trifluoroacetate ZD6474 trifluoroacetate	VEGFR Autophagy Apoptosis	Cancer
Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC₅₀=40 nM). Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC₅₀=110 nM) and *EGFR/HER1* (IC₅₀=500 nM) ^[1].

HY-P99715

Losatuxizumab ABT-806	EGFR	Cancer
Losatuxizumab (ABT-806) is an anti-EGFR monoclonal antibody. Losatuxizumab binds to EGFR with EC₅₀s of 0.96 nM for EGFR wild-type, 0.09 nM for EGFR ^C271A,C283A, 0.12 nM for EGFRvIII, 0.66 nM for EGFR1-501. Losatuxizumab can be used for research of EGFR-expressing cancers ^[1] .

HY-156112

LM2I	Others	Cancer
LM2I is a derivative of Spinosyn A (SPA). LM2I is argininosuccinate synthase (ASS1) enzyme activator, and tumor inhibitor that directly interact with *ASS1. LM2I has significant antiproliferative activity in seven colorectal cancer cell-lines and xenograft tumors of colorectal cancer. LM2I inhibits colorectal cancer cell growth via the EGFR pathway .*

HY-50896S

Erlotinib-d6 CP-358774-d₆; NSC 718781-d₆; OSI-774-d₆	EGFR	Cancer
Erlotinib-d₆ (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 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-10260S1

Vandetanib-d4	Isotope-Labeled Compounds VEGFR Autophagy Apoptosis	Cancer
Vandetanib-d₄ is the deuterium labeled Vandetanib. Vandetanib (ZD6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1][2].

HY-10260S

Vandetanib-d6 ZD6474-d₆	Isotope-Labeled Compounds VEGFR Autophagy Apoptosis	Cancer
Vandetanib-d₆ is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1].

HY-116624

MAZ51 2 Publications Verification	VEGFR Apoptosis	Cancer
MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity ^[1] .

HY-149695

EGFR-IN-91	EGFR	Cancer
EGFR-IN-91 (compound 9) is an orally available *EGFR* inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR ^L858R/C797S and EGFR ^{exon 19del/C797S}, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .

HY-15196

TAK-285 2 Publications Verification	EGFR	Cancer
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and *EGFR(HER1)* inhibitor with IC₅₀ of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for *HER1/2* than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity ^[1]. TAK-285 can cross the blood-brain barrier (BBB) .

HY-156470

Multi-kinase-IN-6	Trk Receptor Anaplastic lymphoma kinase (ALK) c-Kit EGFR Pim Casein Kinase Checkpoint Kinase (Chk) CDK Apoptosis	Cancer
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, *EGFR, PIM1*, CK2α, *CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC₅₀* values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect ^[1].

Serclutamab PR-1594407; DC-1630423	EGFR	Others
Serclutamab is a humanized chimeric antibody targeting EGFR IgG1-κ. Mainly expressed by CHO (Chinese Hamster Ovary) cells ^[1].

Losatuxizumab ABT-806	EGFR	Cancer
Losatuxizumab (ABT-806) is an anti-EGFR monoclonal antibody. Losatuxizumab binds to EGFR with EC₅₀s of 0.96 nM for EGFR wild-type, 0.09 nM for EGFR ^C271A,C283A, 0.12 nM for EGFRvIII, 0.66 nM for EGFR1-501. Losatuxizumab can be used for research of EGFR-expressing cancers ^[1] .

Erlotinib-13C6
Erlotinib- ¹³C₆ is a ¹³C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1].

Erlotinib-d6
Erlotinib-d₆ (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Vandetanib-d4
Vandetanib-d₄ is the deuterium labeled Vandetanib. Vandetanib (ZD6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1][2].

Vandetanib-d6
Vandetanib-d₆ is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1].

Erlotinib-13C6 CP-358774-¹³C₆; NSC 718781-¹³C₆; OSI-774-¹³C₆		Alkynes
Erlotinib- ¹³C₆ is a ¹³C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1].

Erlotinib-d6 CP-358774-d₆; NSC 718781-d₆; OSI-774-d₆		Alkynes
Erlotinib-d₆ (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 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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