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Del

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (1) Apoptosis (10) Autophagy (8) CFTR (16) E1/E2/E3 Enzyme (1) EGFR (41) ERK (1) Histone Methyltransferase (2) PROTACs (4)
By Research Areas:	Cancer (47) Endocrinology (7) Inflammation/Immunology (5)

Inhibitors & Agonists

Recombinant Proteins

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-18932

DEL-22379 1 Publications Verification	ERK Apoptosis	Cancer
DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a K_d estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC₅₀ of ~0.5 μM.

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-137191

CH7233163	EGFR	Cancer
CH7233163 is a noncovalent ATP-competitive inhibitor for *EGFR*-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities .

HY-19970

KM11060 2 Publications Verification	CFTR Autophagy	Endocrinology
KM11060 is a corrector of the F508 deletion (F508del)-cystic fibrosis transmembrane conductance regulator (CFTR) trafficking defect. KM11060 can be used for the research of F508del-CFTR processing defect and development of cystic fibrosis research .

HY-13017S

Ivacaftor-d9 VX-770-d₉	CFTR	Cancer
Ivacaftor-d₉ is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research[1].

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-143445

EGFR-IN-48	EGFR	Cancer
EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC₅₀s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR ^d19/TM/CS, EGFR ^LR/TM/CS, EGFR ^WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3 ^{EGFR del19/T790M/C797S} and PC-9 ^{EGFR del19/T790M/C797S} cells with IC₅₀s of 1.526, 66.7 nM, respectively .

HY-142517

EGFR-IN-25	EGFR	Cancer
EGFR-IN-25 is a potent EGFR inhibitor with IC₅₀s of 9 nM and 60 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and A431 cells (WT), respectively .

HY-142519

EGFR-IN-27	EGFR	Cancer
EGFR-IN-27 is a potent EGFR inhibitor with IC₅₀s of <50 nM for EGFR Del, L858R, Del/T790M, L858R/T790M, Del/T790M/C797S, and L858R/T790M/C797S, respectively (WO2021249324A1, compound 511) .

HY-13017S1

Ivacaftor-d19 VX-770-d₁₉	CFTR Autophagy	Endocrinology
Ivacaftor-d₉ is a potent CFTR modulator and exhibits an EC₅₀ value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research .

HY-156284

EGFR-IN-89	EGFR	Cancer
EGFR-IN-89 (compound 13k) is a potent, fourth-generation EGFR mutation inhibitor with an IC₅₀ of 10.1 nM against Del19/T790M/C797S mutations. EGFR-IN-89 shows higher selectivity over wild type .

HY-15448

Tezacaftor Maximum Cited Publications 13 Publications Verification VX-661	CFTR	Cancer
Tezacaftor (VX-661) is a F508del CFTR corrector. It helps CFTR protein reach the cell surface. However, Ivacaftor (VX-770, HY-13017), a CFTR potentiator, helps to prolong the opening time of cell surface CFTR protein channels. Tezacaftor combining with Ivacaftor, shows potent efficacy against cystic fibrosis and diseases with homozygous for the CFTR Phe508del mutation. Moreover, Elexacaftor (VX-445, HY-111772) is also a CFTR corrector. Elexacaftor-Tezacaftor-Ivacaftor aims at with cystic fibrosis (CF) with at least one Phe508del mutation, often avoids the indication for lung transplantation .

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-151882

EGFR-IN-73	EGFR	Cancer
EGFR-IN-73 (Compound 3f) is a potent inhibitor for the most common EGFR mutation EGFR Del19 with an IC₅₀ of 119 nM .

HY-163094

EGFR-IN-95	EGFR	Cancer
EGFR-IN-95 (compound 5j) is an 2,4-diaminonicotinamide derivative. EGFR-IN-95 has potent inhibitory activity against EGFR del19/T790M/C797S and L858R/T790M/C797S .

HY-111099

GLPG1837 ABBV-974	CFTR Autophagy	Others
GLPG1837 is a potent and reversible CFTR potentiator, with EC₅₀s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.

HY-161126

EGFR-IN-98	EGFR	Cancer
EGFR-IN-98 (Compound 4c) is a EGFR inhibitor. The IC₅₀ values of L858R/T790M/C797S and Del19/T790M/C797S are 0.277 μM and 0.089 μM, respectively. EGFR-IN 98 can be used in the study of tumors .

HY-162881

DS06652923	EGFR	Cancer
DS06652923 is an orally active EGFR triple mutation inhibitor. DS06652923 has a growth inhibition effect on Ba/F3 EGFR del19/T90M/C797S cells, with a GI₅₀ value of 9.4 nM. DS06652923 can lead to tumor regression in Ba/F3 xenograft models .

HY-161319

EGFR-IN-104	EGFR	Cancer
EGFR-IN-104 (Compound A23) is an effective inhibitor of EGFR, with IC₅₀ values of 0.33 μM and 0.133 μM against EGFR ^L858R/T790M and EGFR ^{Del19/T790M/C797S}, respectively. EGFR-IN-104 exhibits anticancer activity both in vitro and in vivo .

HY-158002

IDOR-4	CFTR	Inflammation/Immunology
IDOR-4 is a type IV CFTR corrector. IDOR-4 restores F508del-CFTR trafficking to the cell surface .

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-119936

GLPG2451	CFTR Autophagy	Inflammation/Immunology
GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator, which effectively potentiates low temperature rescued F508del CFTR with an EC₅₀ of 11.1 nM .

HY-123967

RNF5 inhibitor inh-02	E1/E2/E3 Enzyme	Inflammation/Immunology
RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 leads to significant F508del-CFTR rescue (EC₅₀=2.2 uM) in bronchial epithelial cells homozygous for the F508del mutation. RNF5 inhibitor inh-02 can be used for cystic fibrosis research .

HY-157166

EGFR kinase inhibitor 2	EGFR	Cancer
EGFR kinase inhibitor 2 (compound A-7) is a potent EGFR inhibitor targeting EGFR ^{L858R/T790M/C797S} and EGFR ^{Del19/T790M/C797S} mutants. EGFR kinase inhibitor 2 has the potential to address acquired resistance in the treatment of non-small cell lung cancer .

HY-15448A

(Rac)-Tezacaftor (Rac)-VX-661	CFTR	Inflammation/Immunology
(Rac)-Tezacaftor ((Rac)-VX-661) is a racemate of Tezacaftor (HY-15448). Tezacaftor is a F508del CFTR corrector. (Rac)-Tezacaftor can be used for the research of cystic fibrosis .

HY-13017

Ivacaftor 5+ Cited Publications VX-770	CFTR Autophagy	Endocrinology
Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC₅₀s of 100 nM and 25 nM, respectively.

HY-139611C

MRTX-1719 hydrochloride	Histone Methyltransferase	Cancer
MRTX-1719 hydrochloride is a potent first-in-class selective inhibitor of the PRMT5/MTA complex, with an IC₅₀ of less than 10 nM in PRMT5/MTA MTAP ^DEL SDMA cells .

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-15448S

Tezacaftor-d4 VX-661-d₄	CFTR Autophagy	Cancer
Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor (HY-15448), a F508del CFTR corrector. Tezacaftor helps CFTR protein reach the cell surface .

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-109177

Icenticaftor QBW251	CFTR	Inflammation/Immunology
Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC₅₀s of 79 nM and 497 nM for *F508del* and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research .

HY-149401

EGFR-IN-82	EGFR	Cancer
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC₅₀ values of 0.09 and 0.06 nM for EGFR ^{L858R/T790M/C797S} and EGFR ^{Del19/T790M/C797S}, respectively. EGFR-IN-82 has no significant effect on EGFR ^WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .

HY-19815

Olafertinib	EGFR	Cancer
Olafertinib is a third-generation EGFR TKI, with GI₅₀ values of 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19) and 689 nM (EGFR WT), respectively. Olafertinib has the potential for NSCLC research .

HY-126394B

Bamocaftor potassium VX-659 potassium	CFTR	Endocrinology
Bamocaftor potassium is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector designed to restore *F508del-CFTR* protein function. Bamocaftor potassium can be used combine with Tezacaftor (HY-15448) and Ivacaftor (HY-13017) in cystic fibrosis research .

HY-146423

PROTAC EGFR degrader 6	PROTACs EGFR Apoptosis	Cancer
PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFR ^Del19 in HCC827 cells with the DC₅₀ of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase .

HY-126394

Bamocaftor VX-659	CFTR	Endocrinology
Bamocaftor (VX-659) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector designed to restore *F508del-CFTR* protein function. Bamocaftor can be used combine with Tezacaftor (HY-15448) and Ivacaftor (HY-13017) in cystic fibrosis research .

HY-146422

PROTAC EGFR degrader 5	PROTACs EGFR Apoptosis	Cancer
PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFR ^Del19 in HCC827 cells with the DC₅₀ of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase .

HY-142680

EGFR-IN-23	EGFR	Cancer
EGFR-IN-23 is a potent EGFR TKI (tyrosine kinase inhibitor) with an IC₅₀ of 8.05 nM for BaF3/EGFR-DEL19/T790M/C797S cell (WO2021244502A1, compound 8) .

HY-13017S2

Ivacaftor-d18 VX-770-d₁₈	Autophagy CFTR	Endocrinology
Ivacaftor-d₁₈ is the deuterium labeled Ivacaftor[1]. Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively[2].

HY-161275

BI-4732	EGFR	Cancer
BI-4732 a potent inhibitor EGFR-activating (E19del and L858R) and T790M mutations, with high blood-brian barrier penetration, targeting a broad range of EGFR mutations, including C797S. BI-4732 has anti-tumor activity .

HY-164000

CFTR corrector 15	CFTR	Others
CFTR corrector 15 (Compound 4172) is a corrector for cystic fibrosis transmembrane conductance regulator (CFTR), that repairs the F508del-CFTR folding defect when used with VX-809 (HY-13262). CFTR corrector 15 can be used in research of cystic fibrosis disease .

HY-123921

Gefitinib-based PROTAC 3 2 Publications Verification	PROTACs EGFR	Cancer
Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a von Hippel-Lindau ligand via a linker, induces EGFR degradation with DC₅₀s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively .

HY-157432

EGFR-IN-97	EGFR Apoptosis	Cancer
EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFR ^{L858R/T790M/C797S} and Ba/F3-EGFR ^{Del19/T790M/C797S} cells, with IC₅₀ values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFR ^{L858R/T790M/C797S} cells at the concentration of 0.8 μM .

HY-142512

EGFR-IN-24	EGFR	Cancer
EGFR-IN-24, a potent EGFR inhibitor, shows inhibition against EGFR(del19/T790M/C797S) and EGFR(L858R/T790M/C797S), respectively .

HY-13017S3

Ivacaftor-d4 VX-770-d4	CFTR	Endocrinology
Ivacaftor-d4 (VX-770-d4) is the deuterium labeled-Ivacaftor (HY-13017). Ivacaftor is a potent and orally active CFTR potentiator, targeting G551D-CFTR and *F508del-CFTR* with EC₅₀s of 100 nM and 25 nM, respectively .

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-18750A

Zorifertinib hydrochloride AZD3759 hydrochloride	EGFR Apoptosis	Cancer
Zorifertinib (AZD3759) hydrochloride is a potent, orally active, central nervous system-penetrant, EGFR inhibitor (IC₅₀s: 0.3, 0.2, and 0.2 nM for EGFR ^wt, EGFR ^L858R, and EGFR ^{exon 19Del}, respectively). Zorifertinib hydrochloride induces cancer cell apoptosis. Zorifertinib hydrochloride has antitumor activity, and can be used for NSCLC, HCC etc. research .

HY-164490

LS-106	EGFR Apoptosis	Cancer
LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR ^{19del/T790M/C797S} and EGFR ^{L858R/T790M/C797S} with IC₅₀ values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR ^{19del/T790M/C797S} and leas to significant tumor regression in a C797S-mutant xenograft model .

HY-18750

Zorifertinib 5+ Cited Publications AZD3759	EGFR Apoptosis	Cancer
Zorifertinib (AZD3759) is a potent, orally active, central nervous system-penetrant, EGFR inhibitor. At K_m ATP concentrations, the IC₅₀s are 0.3, 0.2, and 0.2 nM for EGFR ^wt, EGFR ^L858R, and EGFR ^{exon 19Del}, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research .

HY-138072

EMI1	EGFR	Cancer
EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC) .

Cat. No.	Compare	Product Name	Species	Source

HY-P703439

	*RAD51 Protein, Pyrococcus furiosus(del* R288-G301)** DNA repair and recombination protein RadA; radA; Pyrococcus furiosus (strain ATCC 43587 / DSM 3638 / JCM 8422 / Vc1); DNA-binding	Others	E. coli
	RAD51 Protein, Pyrococcus furiosus(del R288-G301) is the recombinant RAD51, expressed by E. coli , with tag Free labeled tag. ,

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Cat. No.	Product Name	Chemical Structure

HY-13017S

Ivacaftor-d9
Ivacaftor-d₉ is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research[1].

HY-15448S

Tezacaftor-d4
Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor (HY-15448), a F508del CFTR corrector. Tezacaftor helps CFTR protein reach the cell surface .

HY-13017S3

Ivacaftor-d4
Ivacaftor-d4 (VX-770-d4) is the deuterium labeled-Ivacaftor (HY-13017). Ivacaftor is a potent and orally active CFTR potentiator, targeting G551D-CFTR and *F508del-CFTR* with EC₅₀s of 100 nM and 25 nM, respectively .

HY-13017S1

Ivacaftor-d19
Ivacaftor-d₉ is a potent CFTR modulator and exhibits an EC₅₀ value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research .

HY-13017S2

Ivacaftor-d18
Ivacaftor-d₁₈ is the deuterium labeled Ivacaftor[1]. Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively[2].

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