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Results for "

T790M/Del

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (4) Anaplastic lymphoma kinase (ALK) (2) Apoptosis (10) Autophagy (1) Cannabinoid Receptor (1) Caspase (1) Cytochrome P450 (1) Drug Intermediate (1) EGFR (36) ERK (2) Ferroptosis (1) Glutathione Peroxidase (1) JAK (1) p38 MAPK (2) PROTACs (2) Reactive Oxygen Species (ROS) (1) Reference Standards (1) Ribosomal S6 Kinase (RSK) (1) STAT (1)
By Research Areas:	Cancer (37) Inflammation/Immunology (2)

Inhibitors & Agonists

Biochemical Assay Reagents

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-112823

Almonertinib Maximum Cited Publications 9 Publications Verification HS-10296	EGFR	Cancer
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC₅₀: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .

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-156698

HJM-561	PROTACs EGFR	Cancer
HJM-561 is a selective and effective orally active EGFR PROTAC degrader. HJM-561 is able to overcome the triple EGFR mutations that are resistant to Osimertinib (HY-15772). HJM-561 exhibits potent degradation of EGFR Del19/T790M/C797S (DC₅₀: 9.2 nM) and L858R/T790M/C797S (DC₅₀: 5.8 nM), and has anti-tumor activity (pink: EGFR ligand (HY-12857); blue: CRBN ligand (HY-A0003); black: linker) .

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-112823A

Almonertinib mesylate Maximum Cited Publications 9 Publications Verification HS-10296 mesylate	EGFR	Cancer
Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC₅₀: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .

HY-112823B

Almonertinib hydrochloride Maximum Cited Publications 9 Publications Verification HS-10296 hydrochloride	EGFR	Cancer
Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC₅₀: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .

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-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-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-161275

BI-4732	EGFR Akt ERK Ribosomal S6 Kinase (RSK)	Cancer
BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC₅₀ values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring *EGFR*_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .

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-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-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) .

HY-150610

EGFR-IN-69	EGFR	Cancer
EGFR-IN-69 (compound 17g) is a potent EGFR inhibitor, with IC₅₀ values of 4.3, 6.6 and 25.6 nM against EGFR ^{L858R/T790M/C797S}, EGFR ^L858R/T790M, and EGFR ^{19del/T790M/C797S}, respectively. EGFR-IN-69 can be used for non-small-cell-lung-cancer (NSCLC) research .

HY-164392

TAS-121	EGFR Apoptosis	Cancer
TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC₅₀=1.7 nM), Ex19del mutation (IC₅₀=2.7 nM), L858R/T790M mutation (IC₅₀=0.56 nM) and Ex19del/T790M mutation (IC₅₀=1.1 nM) and wild-type EGFR (IC₅₀=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC₅₀s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models .

HY-175864

EGFR-IN-173	EGFR Apoptosis p38 MAPK ERK Akt STAT	Inflammation/Immunology Cancer
EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR ^{19del/T790M/C797S} with an IC₅₀ of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC₅₀ = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research .

HY-178057

EGFR-IN-176	EGFR Akt Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR ^{19del/T790M/C797S} and EGFR ^{L858R/T790M/C797S}. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC₅₀ < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC) .

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-112823R

Almonertinib (Standard) HS-10296 (Standard)	Reference Standards EGFR	Cancer
Almonertinib (Standard) is the analytical standard of Almonertinib. This product is intended for research and analytical applications. Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC₅₀: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .

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-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-170497

EGFR-IN-140	EGFR	Cancer
EGFR-IN-140 (Compound 31) is the inhibitor for EGFR, that inhibits EGFR wildtype and EGFR L858R/T790M/C797S mutant with K_i of 0.95 nM and 2.1 nM, and inhibits EGFR del19/T790M/C797S in Ba/F3 with an IC₅₀ of 56.9 nM. EGFR-IN-140 exhibits antitumor efficacy in mouse model .

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-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-172795

EGFR-IN-158	EGFR Apoptosis	Cancer
EGFR-IN-158 (compound 12e) is an orally active EGFR inhibitor with an IC₅₀ of 0.22 nM for EGFR(Del19/T790M). EGFR-IN-158 inhibits phosphorylation and downstream signaling by binding to EGFR, thereby inhibiting the proliferation of tumor cell lines and promoting apoptosis .

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-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-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-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-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-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-178448

EGFR-IN-178	EGFR JAK Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Cannabinoid Receptor Glutathione Peroxidase Caspase	Inflammation/Immunology Cancer
EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC₅₀ = 3.4 nM), L858R/T790 M (IC₅₀ = 2.9 nM), and Del19/T790 M (IC₅₀ = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC₅₀ = 55.6 nM) and JAK3 (IC₅₀ = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC) .

HY-161785

EGFR-IN-117	Apoptosis EGFR	Cancer
EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFR ^{L858R/T790M/C797S} and BaF3– ^{C797S/Del19/T790M}, with IC₅₀ of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models .

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-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-170928

DA-0157	EGFR Anaplastic lymphoma kinase (ALK) Cytochrome P450	Cancer
DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC₅₀ = 6.9 nM), Ba/F3-EGFR WT (IC₅₀ = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC₅₀ = 5.5 nM), and Ba/F3-EML4-ALK (IC₅₀ = 7.4 nM). DA-0157 inhibits CYP2D6 with IC₅₀ of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models .

HY-183277

EGFR-IN-209	EGFR p38 MAPK Akt Apoptosis	Cancer
EGFR-IN-209 (Compound 6g) is an orally active, selective EGFR ^{Del19/T790M/C797S} inhibitor with an IC₅₀ of 0.056 μM. EGFR-IN-209 blocks the phosphorylation of EGFR and its downstream effector molecules (pMAPK, pAKT). EGFR-IN-209 induces Apoptosis. EGFR-IN-209 exhibits antitumor activity against Osimertinib (HY-15772)-resistant non-small cell lung cancer. EGFR-IN-209 can be used in research related to non-small cell lung cancer .

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 .

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