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Mutant EGFR inhibitor

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By Targets:	EGFR (92) Akt (1) Anaplastic lymphoma kinase (ALK) (2) Antibody-Drug Conjugates (ADCs) (1) Apoptosis (11) Autophagy (1) BMX Kinase (1) Btk (2) Cytochrome P450 (1) ERK (1) Estrogen Receptor/ERR (1) FAK (2) GSK-3 (1) Isotope-Labeled Compounds (1) MEK (1) mTOR (1) PD-1/PD-L1 (1) Phosphatase (1) PROTACs (9) SHP2 (1) TAM Receptor (1) Trk Receptor (1)
By Research Areas:	Cancer (98) Inflammation/Immunology (1)
Click Chemistry:	Alkynes (4)

101

Inhibitors & Agonists

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: EGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13984

**Mutant EGFR inhibitor**	EGFR	Cancer
Mutant EGFR inhibitor is a potent and selective mutant *EGFR* inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR ^L858R, EGFR ^{Exon 19 deletion} and EGFR ^T790M.

HY-19803

Naquotinib mesylate 4 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-19729

Naquotinib 4 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-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-131066

EMI48	EGFR	Cancer
EMI48, the derivative of EMI1, displays greater potency toward mutant *EGFR* than EMI1. EMI48 inhibits *EGFR* triple mutants .

HY-131067

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

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 .

HY-100520

EGFR-IN-2	EGFR	Cancer
EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation *EGFR* inhibitor.

HY-128860

Mutated EGFR-IN-2	EGFR	Cancer
Mutated EGFR-IN-2 (compound 91) is a mutant-selective *EGFR* inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC₅₀=＜1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity .

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-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-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-161030

EGFR-IN-92	EGFR	Cancer
EGFR-IN-92 (compound 15) is an allosteric T790M/L858R double mutant EGFR inhibitor. EGFR-IN-92 shows antiproliferative activity against H1975 non-small lung cancer (NSCLC) cancer cells expressing double mutant EGFR .

HY-12872A

Nazartinib mesylate EGF816 mesylate	EGFR	Cancer
Nazartinib mesylate (EGF816 mesylate) is a novel, 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-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-157229

STX-721	EGFR	Others
STX-721 is a mutant-selective inhibitor of EGFR and HER2 Exon 20 insertion (ex20ins) 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-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 .

HY-157526

EGFR-TK-IN-1	EGFR Apoptosis	Cancer
EGFR-TK-IN-1 (compound 7o) is a potent mutant *EGFR* inhibitor with IC₅₀ of 8.5 nM an 9.3 nM against EGFR ^L858R/T790M and EGFR ^Del19.EGFR-TK-IN-1 showes strong antiproliferative effects against EGFR mutant-driven non-small cell lung cancer (NSCLC) cells and induces cell apoptosis .

HY-19617

EGFR-IN-1	EGFR	Cancer
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 .

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 .

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-125841

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

HY-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-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-18213

EGFR-IN-9	EGFR	Cancer
EGFR-IN-9 (Compound 8) is a potent EGFR kinase inhibitor with IC₅₀s 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-161031

EGFR-IN-93	EGFR	Cancer
EGFR-IN-93 (compound 18) is an allosteric inhibitor of T790M/L858R double mutant *EGFR. EGFR*-IN-93 can be used for non-small lung cancer (NSCLC) research .

HY-161602

EGFR/HER2-IN-13	EGFR	Cancer
EGFR/HER2-IN-13 (Compd 38) is an inhibitor of **mutant EGFR/HER2s** which are resistant to other drugs. EGFR/HER2-IN-13 can be used for cancer research .

HY-161603

EGFR/HER2-IN-14	EGFR	Cancer
EGFR/HER2-IN-14 (Compd 46) is an inhibitor of **mutant EGFR/HER2s** which are resistant to other drugs. EGFR/HER2-IN-14 can be used for cancer research .

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-79077

Osimertinib dimesylate Maximum Cited Publications 102 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-139884

EGFR-IN-18	EGFR	Cancer
EGFR-IN-18 potently inhibits enzymatic activity in L858R/T790M/C797S mutant *EGFR* (4.9 nM), with a significantly lower activity for wild-type *EGFR* (47 nM).

HY-141640

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

HY-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 .

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-100213

EAI045 1 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-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-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-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-168112

EGFR-IN-127	EGFR	Cancer
EGFR-IN-127 is an ATP-competitive EGFR inhibitor with IC₅₀s of 136.3 nM and 161. 2 nM for EGFR ^del19 and EGFR ^{del19/T790M/C797S}, respectively. EGFR-IN-127 has the potential for the study of non-small-cell lung cancer (NSCLC) .

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-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-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-156712

Depatuxizumab MMAE	Antibody-Drug Conjugates (ADCs)	Cancer
Depatuxizumab MMAE is an antibody-drug conjugate (ADC) comprising an anti EGFR monoclonal antibody (Depatuxizumab) and the cytotoxic agent Monomethyl auristatin E (MMAE). Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR .

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-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-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-15164

Icotinib Hydrochloride 5+ Cited Publications BPI-2009H	EGFR	Cancer
Icotinib Hydrochloride (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 (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-15164A

Icotinib 5+ Cited Publications BPI-2009	EGFR	Cancer
Icotinib (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 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Cat. No.	Product Name	Target	Research Area

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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-P99849

Depatuxizumab ABT-806	Classification of Application Fields Disease Research Fields Cancer	EGFR
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 .

Cat. No.	Product Name	Chemical Structure

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[1].

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-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.

Cat. No.	Product Name		Classification

HY-15164

Icotinib Hydrochloride 5+ Cited Publications BPI-2009H		Alkynes
Icotinib Hydrochloride (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 (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-15164A

Icotinib 5+ Cited Publications BPI-2009		Alkynes
Icotinib (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 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-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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Mutant EGFR inhibitor

Inhibitors & Agonists

Inhibitory Antibodies

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Isotope-Labeled Compounds

Click Chemistry

Natural
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