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Isoforms Recommended:	EGFR/ErbB1/HER1

Results for "

EGFRL858R

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (3) Apoptosis (6) Autophagy (5) c-Met/HGFR (2) EGFR (27) Isotope-Labeled Compounds (1) p38 MAPK (2) PERK (1) PI3K (1) PROTACs (1) Reference Standards (9)
By Research Areas:	Cancer (28) Neurological Disease (1)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-10261R

Afatinib (Standard) BIBW 2992 (Standard)	Reference Standards EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK	Cancer
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .

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-151048

JBJ-07-149	EGFR	Cancer
JBJ-07-149 is an inhibitor for *EGFRL858R/T790M* with an IC₅₀ of 1.1 nM. JBJ-07-149 inhibits the proliferation of cell Ba/F3 with IC₅₀ of 4.9 μM and 0.148 μM, without and with presence of Cetuximab (HY-P9905). JBJ-07-149 can be used as ligand for target protein in synthesis of DDC-01-163 (HY-139997) .

HY-178939

EGFR-IN-181	EGFR Akt PERK Apoptosis	Neurological Disease Cancer
EGFR-IN-181 is an orally active, potent, brain-penetrant *EGFR^{L858R/T790M/C797S}* triple mutations inhibitor (IC₅₀ = 1.32 nM). EGFR-IN-181 can inhibit *EGFR* phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK). EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases .

HY-10261S1

Afatinib-d4 BIBW 2992-d₄	EGFR Autophagy	Cancer
Afatinib-d₄ is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.

HY-79077R

Osimertinib dimesylate (Standard) AZD-9291 dimesylate (Standard); Mereletinib dimesylate (Standard)	EGFR Reference Standards	Cancer
Osimertinib (dimesylate) (Standard) is the analytical standard of Osimertinib (dimesylate). This product is intended for research and analytical applications. Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.

HY-10261AS

Afatinib-d6 dimaleate BIBW 2992MA2-d₆	Isotope-Labeled Compounds EGFR Autophagy	Cancer
Afatinib-d₆ (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC₅₀s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively .

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-B0793S1

AZ-5104-d2	EGFR	Cancer
AZ-5104-d₂ is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC₅₀s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively .

HY-15164R

Icotinib Hydrochloride (Standard) BPI-2009H (Standard)	EGFR Reference Standards	Cancer
Icotinib (Hydrochloride) (Standard) is the analytical standard of Icotinib (Hydrochloride). This product is intended for research and analytical applications. Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFRL858R, EGFRL858R/T790M, EGFRT790M and EGFRL861Q. 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-10261AR

Afatinib dimaleate (Standard) BIBW 2992MA2 (Standard)	Reference Standards EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK	Cancer
Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .

HY-156457

EGFR-IN-90	EGFR	Cancer
EGFR-IN-90 (compound 34) is an orally active *EGFR* inhibitor. EGFR-IN-90 shows inhibitory activity against EGFRL858R/T790M/C797S with an IC₅₀ of 5.1 nM and inhibits the proliferation of the H1975-TM cell line harboring EGFRL858R/T790M/C797S with an IC₅₀ of 0.05 μM. EGFR-IN-90 and inhibits tumor growth in the H1975-TM xenograft tumor model .

HY-142512

EGFR-IN-24	EGFR	Cancer
EGFR-IN-24 is a selective *EGFR* triple mutant inhibitor with >300 nM IC₅₀ against human EGFR^{del19/T790M/C797S}, EGFR^{L858R/T790M/C797S}, and EGFR^WT. EGFR-IN-24 can be used for the research of non-small cell lung cancer .

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-161968

EGFR/PI3Kα-IN-1	EGFR PI3K	Cancer
EGFR/PI3Kα-IN-1 (compound 30k) is a dual EGFR/PI3Kα inhibitor with IC₅₀ values of 3.6 nM (EGFRL858R/T790M) and 30 nM (PI3Kα), respectively. EGFR/PI3Kα-IN-1 can inhibit tumor cell proliferation and has anticancer activity .

HY-147858A

*PROTAC EGFR* degrader 7 diTFA**	PROTACs	Cancer
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC₅₀ of 13 .2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC₅₀ of 46 .82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research .

HY-133780

Afatinib impurity 11	EGFR Autophagy	Cancer
Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible *EGFR* family inhibitor with IC₅₀s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR ^wt, EGFR ^L858R, EGFR ^L858R/T790M and HER2, respectively .

HY-173492

EGFR-IN-156	EGFR Apoptosis	Cancer
EGFR-IN-156 (Compound 7f) is an *EGFR* inhibitor that also has inhibitory activity against mutations EGFRL858R and EGFRT790M (IC₅₀ values are 0.186, 0.131, and 0.107 μM, respectively). EGFR-IN-156 has significant anticancer activity against human cancer cell lines HepG-29 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer) (IC₅₀ values are 1.67, 5.32, and 6.56 μM, respectively). EGFR-IN-156 inhibits cancer cell proliferation by inducing cell cycle arrest at the G/G1 phase and triggering apoptosis. EGFR-IN-156 shows promise in EGFR-related cancers .

HY-100213R

EAI045 (Standard)	EGFR Reference Standards	Cancer
EAI045 (Standard) is the analytical standard of EAI045 (HY-100213). This product is intended for research and analytical applications. 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, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively.

HY-155358

Os30	EGFR Apoptosis	Cancer
Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC₅₀ values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation .

HY-10346AR

AV-412 free base (Standard) MP-412 free base (Standard)	Reference Standards EGFR	Cancer
AV-412 free base (Standard) is the analytical standard of AV-412 free base (HY-10346A). This product is intended for research and analytical applications. AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC₅₀s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.

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-100214R

EAI001 (Standard)	EGFR Reference Standards	Cancer
EAI001 (Standard) is the analytical standard of EAI001 (HY-100214). This product is intended for research and analytical applications. EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer .

HY-162062

EGFR WT/T790M/L858R-IN-1	EGFR	Cancer
EGFR WT/T790M/L858R-IN-1 (compound 10d) is a potent *EGFR* inhibitor, with IC₅₀s of 0.097, 0.280, and 0.051?μM for EGFR ^WT, EGFR ^T790M, and EGFR ^L858R, respectively. EGFR WT/T790M/L858R-IN-1 can be used for the research of cancer .

Cat. No.	Product Name	Chemical Structure

HY-10261S1

Afatinib-d4
Afatinib-d₄ is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.

HY-10261AS

Afatinib-d6 dimaleate
Afatinib-d₆ (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC₅₀s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively .

HY-B0793S1

AZ-5104-d2
AZ-5104-d₂ is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC₅₀s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively .

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