Search Result
Results for "
EGFR mutation
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-16909
-
Leptomycin B
Maximum Cited Publications
21 Publications Verification
CI 940; LMB
|
CRM1
Fungal
Antibiotic
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Infection
Cancer
|
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Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle .
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-
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- HY-132842
-
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DZD9008
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EGFR
Btk
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Cancer
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Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52) .
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-
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- HY-112870
-
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Alflutinib; Furmonertinib; AST2818
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EGFR
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Cancer
|
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Firmonertinib (Alflutinib; Furmonertinib) is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
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-
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- HY-112823
-
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HS-10296
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EGFR
|
Cancer
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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 .
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-
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- HY-135815
-
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TAK-788; AP32788
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EGFR
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Cancer
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Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research .
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-
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- HY-112299
-
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TAS6417; CLN-081
|
EGFR
Apoptosis
|
Cancer
|
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Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM .
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-
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- HY-112870A
-
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Alflutinib mesylate; Furmonertinib mesylate; AST2818 mesylate
|
EGFR
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Inflammation/Immunology
Cancer
|
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Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
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-
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- HY-136789
-
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BDTX-189
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EGFR
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Cancer
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Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity .
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-
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- HY-156698
-
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PROTACs
EGFR
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Cancer
|
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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) .
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- HY-144680
-
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ZL-2313
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EGFR
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Cancer
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BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC) .
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- HY-N1073
-
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6-Isopentenylgenistein; Erythrinin B
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Apoptosis
EGFR
HSP
ERK
Akt
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Infection
Cancer
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Wighteone (6-Isopentenylgenistein; Erythrinin B) is a prenylated isoflavone that acts as a HSP90/EGFR L858R/T790M inhibitor and antifungal agent. Wighteone reduces the expression level of HSP90, blocks EGF-induced phosphorylation of EGFR, and thereby inhibits the downstream ERK and AKT signaling pathways. Wighteone induces cell cycle redistribution, inhibits proliferation and triggers apoptosis in cancer cells. Wighteone can be isolated from Erythrina suberosa, and can also be induced to synthesize in Lotus japonicus under specific conditions. Wighteone can be used to study HER2-positive breast cancer, leukemia, non-small cell lung cancer with EGFR L858R/T790M mutation, and fungal infections .
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- HY-19815
-
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CK-101; RX518
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EGFR
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Cancer
|
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Olafertinib (CK-101) is an orally available, third generation and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Olafertinib selectively inhibits both EGFR-TKI-sensitizing and resistance mutations with minimal activity on wild-type EGFR. Olafertinib can be used in research for non-small cell lung cancer (NSCLC) with EGFR mutations and other advanced malignancies .
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- HY-153268
-
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BDTX-1535; EGFR-IN-76
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EGFR
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
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Silevertinib (BDTX-1535) is an irreversible, brain-penetrant, selective and orally active EGFR inhibitor with wild-type EGFR-sparing. Silevertinib targets key EGFR resistance mutations, including the kinase domain (C797S, L718Q, G724S, S768I), extracellular domain (EGFRvIII, A289X), and EGFR amplification. Silevertinib exerts anti-tumor activity with well tolerated in vivo. Silevertinib can be used for non-small cell lung cancer (NSCLC) and glioblastoma (GBM) research .
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- HY-172429
-
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ORIC-114
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EGFR
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Neurological Disease
Cancer
|
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Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
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- HY-78869
-
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Osimertinib analog
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Drug Derivative
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Infection
Metabolic Disease
Cancer
|
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Mutated EGFR-IN-1 (Osimertinib analog) (Intermediate 168) is a structural analog of Osimertinib (HY-15772) and can be used as a pharmaceutical intermediate for EGFR inhibitors .
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- HY-109189
-
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BPI-7711
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EGFR
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Cancer
|
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Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .
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- HY-137433
-
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D-0316
|
EGFR
P-glycoprotein
Apoptosis
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Cancer
|
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Befotertinib (D-0316) is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFR T790M, EGFR L858R and delE746-A750, forms covalent bonds with EGFR C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib can be used in research related to multidrug-resistant cancers and non-small cell lung cancer .
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- HY-132842A
-
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(S)-DZD9008
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EGFR
Btk
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Cancer
|
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(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK .
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- HY-157229
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STX-721
1 Publications Verification
|
EGFR
ERK
|
Cancer
|
|
STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .
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- HY-112823B
-
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HS-10296 hydrochloride
|
EGFR
|
Cancer
|
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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 .
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- HY-112823A
-
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HS-10296 mesylate
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EGFR
|
Cancer
|
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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 .
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- HY-P99114
-
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PD-1/PD-L1
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Cancer
|
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Sugemalimab is a fully human, full length, anti-programmed death ligand 1 (PD-L1) immunoglobulin G4 (IgG4) monoclonal antibody (mAb). Sugemalimab shows anticancer activities and can be used for non-small cell lung cancer research .
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- HY-134877
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EGFR
ERK
Akt
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Cancer
|
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BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC50 values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits EGFR (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations .
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- HY-135815A
-
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TAK-788 succinate; AP32788 succinate
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EGFR
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Cancer
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Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research .
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- HY-175839
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PROTACs
EGFR
ATP Synthase
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Cancer
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PROTAC EGFR degrader 15 is a Pomalidomide (HY-10984)-based Gefitinib (HY-50895) EGFR PROTAC degrader. PROTAC EGFR degrader 15 triggers EGFR degradation via ubiquitin-proteasome-dependent proteolysis and autophagy-lysosome activation pathways. PROTAC EGFR degrader 15 targets ETFA to enhance ATP production. PROTAC EGFR degrader 15 significantly suppresses tumor growth in a Gefitinib-acquired resistant HCC-827 xenograft model. PROTAC EGFR degrader 15 can be used for the study of non-small cell lung cancer (NSCLC) (Pink: EGFR ligand (HY-W109039); Blue: CRBN ligand (HY-10984); Black: Linker (HY-W679737)) .
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- HY-172429A
-
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ORIC-114 hemihydrate
|
EGFR
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Neurological Disease
Cancer
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Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
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- HY-139997
-
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PROTACs
EGFR
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Cancer
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DDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer .
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- HY-137191
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EGFR
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Cancer
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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 .
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- HY-155537
-
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YK-029A
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EGFR
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Cancer
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YK-029A is an orally active inhibitor of mutant EGFR,targeting to both the T790M mutations (EGFR T790M) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity,and results tumor regression in EGFRex20ins-driven PDX models .
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- HY-D2208
-
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Fluorescent Dye
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Others
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SYTM Green is a cell impermeant DNA dye that fluoresces green by binding to dsDNA (Ex/Em=503/530 nm). SYTM Green can also be used to stain bacteria, including Gram-positive and Gram-negative bacteria. Note: SYTM Green cannot penetrate living cells, and this product is equivalent to (Ex/Em=488/530 nm) .
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- HY-17654
-
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EGFR
mTOR
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Cancer
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BIEGi-1 is an EGFR inhibitor. BIEGi-1 effectively disrupts the EGFR-Rheb interaction in cells. BIEGi-1 robustly inhibits EGFR kinase activity (reduces p-Y1068-EGFR) as well as mTORC1 activation (reduces p-T389-S6K1) in EGFR-mutant cells. BIEGi-1 shows strong antiproliferative effects on EGFR-mutant PC9 and HCC827 cells with IC50 values of 17 nM and 20 nM, respectively. BIEGi-1 can be used for the study of cancers harboring EGFR mutations, such as non-small cell lung cancer (NSCLC) .
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- HY-135887
-
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Anaplastic lymphoma kinase (ALK)
Apoptosis
Autophagy
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Cancer
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ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect .
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- HY-164548
-
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HSP
Apoptosis
PI3K
Akt
NF-κB
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Inflammation/Immunology
Cancer
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WK88-1 is an apoptosis inducer and Hsp90 client protein inhibitor with antiproliferative and immunomodulatory activities. WK88-1 inhibits signaling pathways such as PI3K/Akt and NF-κB, and induces mitochondrial dysfunction and cell cycle arrest. WK88-1 effectively suppresses cancer cell migration and invasion, and reverses various EGFR mutations and resistance to Gefitinib (HY-50895). WK88-1 also regulates the differentiation of monocytes and dendritic cells, blocks the expression of multiple chemokines, inhibits immune cell migration and M1 marker transcription, and restores impaired endocytic activity. WK88-1 has been used in studies of breast cancer, non-small cell lung cancer with various EGFR mutations or Met amplification, and atherosclerosis and other related diseases .
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- HY-175837
-
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EGFR
Apoptosis
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Cancer
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EGFR-IN-172 is a EGFR inhibitor. EGFR-IN-172 effectively inhibits the proliferation of non-small cell lung cancer (NSCLC) cells carrying the L858R, T790M and C797S drug-resistant mutations. EGFR-IN-172 inhibits EGFR phosphorylation, induces cell cycle arrest and apoptosis. EGFR-IN-172 can be used for the study of NSCLC .
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- HY-179143
-
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EGFR
Akt
Apoptosis
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Cancer
|
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EGFR-IN-185 is a EGFR inhibitor. EGFR-IN-185 exhibits potent activity against non-small cell lung cancer (NSCLC) cells harboring EGFR mutations. EGFR-IN-185 inhibits colony formation and migration, induces G0/G1 arrest, and promots apoptosis, which are associated with the suppression of EGFR and AKT phosphorylation. EGFR-IN-185 can be used for the research of NSCLC .
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- HY-144049
-
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EGFR
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Cancer
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EGFR-IN-32 is a potent inhibitor of EGFR. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-32 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185297A1, compound 2) .
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- HY-164392
-
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EGFR
Apoptosis
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Cancer
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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 .
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- HY-156700
-
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PROTAC Linkers
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Cancer
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Lenalidomide-acetylene-Br is a PROTAC Linker taht makes up HJM-561 (HY-156698). HJM-561 is a potent, selective, and orally active EGFR PROTAC to inhiibit Osimertinib (HY-15772)-resistant EGFR triple mutations.
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- HY-P991572
-
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EGFR
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Cancer
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MM-151 is a humanized IgG1 monoclonal antibody targeting EGFR. MM-151 binds multiple regions of the EGFR extracellular domain (ECD) and reduces its mutations in circulating cell-free tumor DNA with EGFR resistance. MM-151 significantly inhibits EGFR signaling and cell growth. MM-151 can be used for drug-resistant cancers research, such as colorectal, non-small cell lung and triple negative breast cancer .
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- HY-178939
-
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EGFR
Akt
PERK
Apoptosis
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Neurological Disease
Cancer
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EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/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 .
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- HY-178057
-
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EGFR
Akt
Anaplastic lymphoma kinase (ALK)
Apoptosis
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Cancer
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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) .
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- HY-175864
-
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EGFR
Apoptosis
p38 MAPK
ERK
Akt
STAT
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Inflammation/Immunology
Cancer
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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 .
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- HY-137433A
-
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D-0316 mesylate
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EGFR
P-glycoprotein
Apoptosis
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Inflammation/Immunology
Cancer
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Befotertinib (D-0316) mesylate is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib mesylate selectively targets EGFR mutations including EGFR T790M, EGFR L858R and delE746-A750, forms covalent bonds with EGFR C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib mesylate inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib mesylate can be used in research related to multidrug-resistant cancers and non-small cell lung cancer .
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- HY-178283
-
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EGFR
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Cancer
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EGFR-IN-177 is a potent EGFR inhibitor with IC50s of 0.32, 1.04, 0.65, 0.67, 0.48, 0.55 and 0.38 nM against EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S, EGFR D746-750, EGFR D746-750/C797S, EGFR D770_N77linsNPG, and EGFR WT. EGFR-IN-177 inhibits lung cancer proliferation and EGFR phosphorylation. EGFR-IN-177 can be used for the study of cancers such as non-small cell lung cancer .
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- HY-144048
-
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EGFR
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Cancer
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EGFR-IN-31 is a potent inhibitor of EGFR. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-31 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185298A1, compound 2) .
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- HY-146262
-
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EGFR
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Cancer
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LDC0496 is a potent and selective EGFR inhibitor. LDC0496 possesses intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations, as well as selectivity over wild type EGFR and within the kinome .
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- HY-144052
-
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EGFR
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Cancer
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EGFR-IN-35 is a potent inhibitor of EGFR. EGFR-IN-35 is an anti-tumor agent with low toxic side effects. EGFR-IN-35 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-35 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 11) .
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- HY-144051
-
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EGFR
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Cancer
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EGFR-IN-34 is a potent inhibitor of EGFR. EGFR-IN-34 is an anti-tumor agent with low toxic side effects. EGFR-IN-35 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-34 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 12) .
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- HY-144056
-
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EGFR
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Cancer
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EGFR-IN-39 is a potent inhibitor of EGFR. EGFR-IN-39 is an anti-tumor agent with low toxic side effects. EGFR-IN-39 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-39 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 2) .
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- HY-144054
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EGFR
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Cancer
|
|
EGFR-IN-37 is a potent inhibitor of EGFR. EGFR-IN-37 is an anti-tumor agent with low toxic side effects. EGFR-IN-39 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-37 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 7) .
|
-
- HY-144055
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-38 is a potent inhibitor of EGFR. EGFR-IN-38 is an anti-tumor agent with low toxic side effects. EGFR-IN-33 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-38 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 4) .
|
-
- HY-144050
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-33 is a potent inhibitor of EGFR. EGFR-IN-33 is an anti-tumor agent with low toxic side effects. EGFR-IN-33 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-33 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 13) .
|
-
- HY-164503
-
|
NEP010
|
EGFR
|
Cancer
|
|
Neptinib (NEP010) is an orally active derivative of Afatinib (HY-10261) that has stronger antitumor activity than Afatinib (HY-10261) by improving pharmacokinetics. Neptinib has a significant inhibitory effect on tumor growth in mouse non-small cell lung cancer models with different EGFR mutations. Neptinib has a certain inhibitory effect on the EGFR kinase family, with IC50 values ??of 0.24 nM, 7.25 nM, 0.46 nM and 1.79 nM for EGFR wt, EGFR L858R/T790M, EGFR L858R and EGFR T790M, respectively .
|
-
- HY-139920A
-
|
SH-1028 mesylate
|
EGFR
|
Cancer
|
|
Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation .
|
-
- HY-162881
-
|
|
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-155358
-
|
|
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-151882
-
|
|
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-156284
-
|
|
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-138627B
-
|
|
EGFR
Drug Metabolite
|
Cancer
|
|
AST5902 mesylate is a principal metabolite of Alflutinib, exhibiting significant antineoplastic activity. AST5902 mesylate contributes to the overall pharmacological effects in the treatment of non-small cell lung cancer. AST5902 mesylate is involved in the response to activating EGFR mutations and can help overcome EGFR T790M drug-resistant mutations.
|
-
- HY-167948
-
|
|
EGFR
|
Cancer
|
|
Dacomitinib metabolite M1/2 is a potent inhibitor of both wild-type (WT) EGFR and the T790M mutation, demonstrating significant activity against acquired resistance mechanisms in EGFR-mutant non-small-cell lung cancer (NSCLC).
|
-
- HY-114253
-
|
|
EGFR
|
Cancer
|
|
ODS-2004436 is a small molecule radiotracer that uses positron emission tomography (PET) imaging to measure the activity of the epidermal growth factor receptor (EGFR) in tumors. ODS-2004436 labeled with the radioactive isotope fluorine-18 shows significantly higher uptake in the xenograft models of lung cancer with EGFR mutations compared to the wild-type models, and could be used to distinguish the mutation status. ODS-2004436 can be used to identify EGFR-positive tumors and predict their response to certain reagent treatments, especially for non-small cell lung cancer (NSCLC) .
|
-
- HY-147994
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research .
|
-
- HY-147992
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research .
|
-
- HY-146210
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells .
|
-
- HY-178824
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-180 (Compound L15) is an EGFR inhibitor. EGFR-IN-180 shows inhibitory activity against EFGR and EGFR harboring the L858R/T790M/C797S triple drug-resistant mutation, with IC50 values of 80.96 nM and 16.43 nM, reapectively. EGFR-IN-180 can be used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-135815B
-
|
TAK-788 mesylate; AP32788 mesylate
|
EGFR
|
Cancer
|
|
Mobocertinib (TAK-788) mesylate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib mesylate can be used in NSCLC research .
|
-
- HY-158178
-
|
|
EGFR
|
Cancer
|
|
EGFR T790M/L858R-IN-7 (Compound 72) is a novel pyrimidine compound that inhibits the EGFR T790M and L858R mutation with a high efficacy (93% inhibition rate at 0.05 μM). EGFR T790M/L858R-IN-7 functions by specifically binding to the kinase domain of EGFR, thereby inhibiting its phosphorylation activity .
|
-
- HY-162299
-
|
|
EGFR
|
Cancer
|
|
EGFR kinase inhibitor 3 (compound 2) is a bivalent ATP-allosteric EGFR kinase inhibitor with IC50s of <10 nM, 1.5 nM, 0.059 nM, 0.064 nM for WT EGFR, EGFR-activating mutations L858R, L858R/T790M and L858R/T790M/C797S, respectively. EGFR kinase inhibitor 3 is a C-linked inhibitor .
|
-
- HY-147826
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR WT, EGFR T790M, EGFR L858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR T790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFR WT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio .
|
-
- HY-161785
-
|
|
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-135815R
-
|
TAK-788 (Standard); AP32788 (Standard)
|
EGFR
Reference Standards
|
Cancer
|
|
Mobocertinib (Standard) is the analytical standard of Mobocertinib. This product is intended for research and analytical applications. Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research .
|
-
- HY-173492
-
|
|
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-164464
-
|
|
EGFR
|
Cancer
|
|
BPI-15086 an orally active, potent, irreversible mutant-selective inhibitor of both EGFR and T790M resistance mutations tyrosine kinase. BPI-15086 can be used for the research of non-small-cell lung cancer .
|
-
- HY-170928
-
|
|
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-172877
-
|
|
Raf
EGFR
Apoptosis
Bcl-2 Family
|
Cancer
|
|
EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual BRAFV600E/EGFR inhibitor with IC50 of 0.048 μM and 0.037 μM, respectively. EGFR/BRAFV600E-IN-5 has significant anti-melanoma activity with IC50 of 3.16 μM and 2.50 μM against MALME-3M and LOX-IMVI cell lines, respectively. EGFR/BRAFV600E-IN-5 exerts anti-tumor effects by inducing G1 arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 can be used for melanoma research, especially for combined inhibition of BRAFV600E mutation and EGFR signaling pathway .
|
-
- HY-173500
-
|
|
MMP
Apoptosis
EGFR
STAT
|
Cancer
|
|
MG-3C is a potent matrix metalloproteinase 9 (MMP-9) inhibitor. MG-3C can selectively kill non-small-cell lung cancer (NSCLC) cells harboring the EGFR T790M mutation. MG-3C blocks the EGFR/STAT3 signaling pathway, inducing G2/M phase arrest, growth inhibition, and apoptosis of cancer cells. MG-3C is promising for research of lung cancer .
|
-
- HY-112823R
-
|
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-147862
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines .
|
-
- HY-147860
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC50 values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.14 and 1.82 μM, respectively .
|
-
- HY-162602
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-115 (H-13) is an EGFR inhibitor, with IC50 of 395.2 nM. EGFR-IN-115 can be used in anti-cancer research .
|
-
- HY-185276
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-204 (Example 1) is a HER2 exon 20 mutation inhibitor with selectivity for wild-type EGFR. EGFR-IN-204 exerts antiproliferative effects on cells dependent on HER2 exon 20 YVMA insertion mutation and wild-type HER2, and shows strong selectivity over cells dependent on wild-type EGFR. EGFR-IN-204 is applicable to non-small cell lung cancer research .
|
-
- HY-112870AS
-
|
Alflutinib-d3 mesylate; Furmonertinib-d3 mesylate; AST2818-d3 mesylate
|
Isotope-Labeled Compounds
EGFR
|
Inflammation/Immunology
Cancer
|
|
Firmonertinib-d3 (Alflutinib-d3) mesylate is the deuterium labeled Firmonertinib mesylate (HY-112870A). Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation.
|
-
- HY-181701
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-202 is an epidermal growth factor receptor (EGFR) inhibitor that selectively targets EGFR exon 20 insertion mutations. EGFR-IN-202 can be used in research related to non-small cell lung cancer .
|
-
- HY-181954
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
ZW-49 is an orally active pan-EGFR inhibitor with IC50 values at 0.03-1.5 nM. ZW-49 inhibits all subgroups of EGFR mutations with selectivity over wild-type EGFR and other target families. ZW-49 blocks the ATP-binding pocket, occupies a conserved hydrophobic subpocket, avoids steric conflicts with PACC mutation P loops. ZW-49 inhibits cancer cells proliferation, induces G0/G1 phase cell-cycle arrest and apoptosis, and demonstrates anti-proliferative activity in xenograft mice models. ZW-49 can be used for the research of cancer, such as non-small cell lung cancer .
|
-
- HY-109189A
-
|
BPI-7711 hydrochloride
|
EGFR
|
Cancer
|
|
Rezivertinib (BPI-7711) hydrochloride is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib hydrochloride exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib hydrochloride has excellent central nervous system (CNS) penetration and has antitumor activity, such as non-small cell lung cancer (NSCLC) .
|
-
- HY-135815AR
-
|
TAK-788 succinate (Standard); AP32788 succinate (Standard)
|
EGFR
Reference Standards
|
Cancer
|
|
Mobocertinib (succinate) (Standard) is the analytical standard of Mobocertinib (succinate). This product is intended for research and analytical applications. Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research .
|
-
- HY-183682
-
|
|
EGFR
p38 MAPK
ERK
Akt
|
Cancer
|
|
AZ14289671 is an orally active, blood-brain barrier-penetrant tyrosine kinase (tyrosine kinase) inhibitor (TKI) that specifically targets non-small cell lung cancer (NSCLC) harboring EGFR exon 20 insertion mutations (EGFR Exon20Ins), while largely sparing wild-type EGFR to reduce off-target toxicities such as rash and diarrhea. AZ14289671 inhibits the downstream MAPK/ERK/AKT pathway, suppressing tumor cell proliferation, survival and migration. AZ14289671 can be used for NSCLC research .
|
-
- HY-109061R
-
|
YH25448 (Standard); GNS-1480 (Standard)
|
Apoptosis
Akt
TRP Channel
EGFR
ERK
Reference Standards
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Lazertinib (Standard) is the analytical standard of Lazertinib (HY-109061). This product is intended for research and analytical applications. Lazertinib (YH25448) is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib can be used in the study of non-small cell lung cancer .
|
-
- HY-109061BR
-
|
YH25448 mesylate (Standard); GNS-1480 mesylate (Standard)
|
Reference Standards
|
Cancer
|
|
Lazertinib mesylate (Standard) is the analytical standard of Lazertinib (mesylate) (HY-109061B). This product is intended for research and analytical applications. Lazertinib (YH25448) mesylate is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib mesylate inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib mesylate can be used in the study of non-small cell lung cancer .
|
-
- HY-18957C
-
|
BGB-283 hydrochloride
|
Endogenous Metabolite
|
Cancer
|
|
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
|
-
- HY-171884
-
|
|
EGFR
|
Cancer
|
|
BI-8128 is a potent EGFR inhibitor, with IC50 values of 12, 6.7, 22, 10, and 3 nM against wild-type, T790M, C797S, T790M/C797S, and L858R/T790M/C797S mutant EGFR, respectively. BI-8128 significantly inhibits the proliferation of Ba/F3 and PC-9 drug-resistant mutant cells. BI-8128 is applicable for the research of non-small cell lung cancer .
|
-
- HY-181542
-
|
|
Aldose Reductase
|
Cancer
|
|
SG-55 is a selective, noncompetitive and orally active AKR1C3 inhibitor with an IC50 of 5 nM and a Ki of 10 nM. SG-55 shows >2000-fold selectivity for AKR1C3 over AKR1C1, AKR1C2, and AKR1C4 (> 10 μM). SG-55 increases the ratio of reduced/oxidized nicotinamide adenine dinucleotide phosphate (NADPH/NADP +), decreases the ratio of reduced/oxidized glutathione (GSH/GSSG), and induces DNA double-strand breaks. SG-55 can overcome Osimertinib (HY-15772) resistance mediated by EGFR C797S triple mutation in non-small cell lung cancer (NSCLC) .
|
-
-
-
HY-L075
-
|
|
2,886 compounds
|
|
Lung cancer is a major global health problem, as it is the leading cause of cancer-related deaths worldwide. Lung cancer is divided into two categories: small cell lung cancer and non-small cell lung cancer (NSCLC). Non-small cell lung cancer accounts for about 85 percent of lung cancers.
As with all cancers, lung cancer may be treated with surgery, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. Targeted therapy is one of the most exciting developments in lung cancer medicine, especially for NSCLC. Extensive genomic characterization of NSCLC has led to the identification of molecular subtypes of NSCLC that are oncogene addicted and exquisitely sensitive to targeted therapies. These include activating mutations in epidermal growth factor receptor (EGFR) and BRAF or echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) fusions and ROS1 receptor tyrosine kinase fusions. These are important targets for target therapy.
MCE offers a unique collection of 2,886 compounds with identified and potential anti-lung cancer activity. These compounds target lung cancer’s major targets and signaling pathways. MCE anti-lung cancer compound library is a useful tool for anti-lung cancer drugs screening and other related research.
|
| Cat. No. |
Product Name |
Type |
-
- HY-D2208
-
|
|
Fluorescent Dyes
|
|
SYTM Green is a cell impermeant DNA dye that fluoresces green by binding to dsDNA (Ex/Em=503/530 nm). SYTM Green can also be used to stain bacteria, including Gram-positive and Gram-negative bacteria. Note: SYTM Green cannot penetrate living cells, and this product is equivalent to (Ex/Em=488/530 nm) .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99114
-
|
|
PD-1/PD-L1
|
Cancer
|
|
Sugemalimab is a fully human, full length, anti-programmed death ligand 1 (PD-L1) immunoglobulin G4 (IgG4) monoclonal antibody (mAb). Sugemalimab shows anticancer activities and can be used for non-small cell lung cancer research .
|
-
(5)
-
- HY-P991572
-
|
|
EGFR
|
Cancer
|
|
MM-151 is a humanized IgG1 monoclonal antibody targeting EGFR. MM-151 binds multiple regions of the EGFR extracellular domain (ECD) and reduces its mutations in circulating cell-free tumor DNA with EGFR resistance. MM-151 significantly inhibits EGFR signaling and cell growth. MM-151 can be used for drug-resistant cancers research, such as colorectal, non-small cell lung and triple negative breast cancer .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N1073
-
|
6-Isopentenylgenistein; Erythrinin B
|
Leguminosae
Genista ephedroides DC.
Plants
Isoflavones
Source Classification
|
Apoptosis
EGFR
HSP
ERK
Akt
|
Wighteone (6-Isopentenylgenistein; Erythrinin B) is a prenylated isoflavone that acts as a HSP90/EGFR L858R/T790M inhibitor and antifungal agent. Wighteone reduces the expression level of HSP90, blocks EGF-induced phosphorylation of EGFR, and thereby inhibits the downstream ERK and AKT signaling pathways. Wighteone induces cell cycle redistribution, inhibits proliferation and triggers apoptosis in cancer cells. Wighteone can be isolated from Erythrina suberosa, and can also be induced to synthesize in Lotus japonicus under specific conditions. Wighteone can be used to study HER2-positive breast cancer, leukemia, non-small cell lung cancer with EGFR L858R/T790M mutation, and fungal infections .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-112870AS
-
|
|
|
Firmonertinib-d3 (Alflutinib-d3) mesylate is the deuterium labeled Firmonertinib mesylate (HY-112870A). Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation.
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-181701
-
|
|
|
Alkynes
|
|
EGFR-IN-202 is an epidermal growth factor receptor (EGFR) inhibitor that selectively targets EGFR exon 20 insertion mutations. EGFR-IN-202 can be used in research related to non-small cell lung cancer .
|
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