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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
164 Results for "
Mutant EGFR inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (164)
164 Results for "Mutant EGFR inhibitor" in MCE Product Catalog:
202
202 Publications Verification
Synonyms: AZD-9291; Mereletinib
Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
202
202 Publications Verification
Cat. No.: HY-79077
CAS No.: 2070014-82-1
Synonyms: AZD-9291 dimesylate; Mereletinib dimesylate
Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
202
202 Publications Verification
Synonyms: AZD-9291 mesylate; Mereletinib mesylate
Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
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Research Areas:
Idasanutlin (RG7388) is an orally bioavailable MDM2 inhibitor with an IC50 of 6 nM. Idasanutlin disrupts MDM2-p53 binding, stabilizes and activates p53, triggering cell cycle arrest, apoptosis, and reduced cancer cell viability. Idasanutlin reduces EGFR protein expression and phosphorylation, suppresses downstream SHP2, MEK1/2, ERK1/2, AKT, mTOR, p70(S6K1), and S6 signaling. Idasanutlin induces mitochondrial ROS production, drives p38 MAPK phosphorylation, upregulates NOXA, and mediates caspase-3-dependent apoptosis and gasdermin E-mediated pyroptosis. Idasanutlin can be used for the research of TP53-mutant non-small cell lung cancer, T-cell acute lymphoblastic leukemia, colorectal carcinoma, melanoma, diffuse large B-cell lymphoma, mantle cell lymphoma, non-Hodgkin lymphoma, severe fever with thrombocytopenia syndrome, neuroblastoma, acute lymphoblastic leukemia, relapsed or refractory acute myeloid leukemia, osteosarcoma, solid tumors, and hematological tumors .
14
14 Cited Publications
Synonyms: CO-1686; AVL-301; CNX-419
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.
14
14 Cited Publications
Synonyms: CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide
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.
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9
Target:
Research Areas:
Icotinib (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
9
Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min −1 on EGFR(L858R/790M) mutant, respectively.
9
Target:
Research Areas:
Icotinib Hydrochloride (BPI-2009) is a potent, CNS-penetrant and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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6 Cited Publications
Synonyms: Alflutinib; Furmonertinib; AST2818
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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6 Cited Publications
Synonyms: Alflutinib mesylate; Furmonertinib mesylate; AST2818 mesylate
Target:
Research Areas:
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 .
5
Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
5
Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
4
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) .
4
4 Cited Publications
Cat. No.: HY-N2445
CAS No.: 37308-75-1
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3 Cited Publications
EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR L858R, EGFR T790M and EGFR L858R/T790M at 10 μM ATP, respectively.
3
3 Cited Publications
Synonyms: YH25448; GNS-1480
Target:
Research Areas:
Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
3
3 Cited Publications
Cat. No.: HY-109061B
CAS No.: 2247995-37-3
Synonyms: YH25448 mesylate; GNS-1480 mesylate
Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
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2 Cited Publications
Synonyms: EGFR Mutant-IN-3
Target:
Research Areas:
NT-1 (EGFR mutant-IN-3) is a potent mutant EGFR inhibitor and an analog of Osimertinib (HY-15772). This mutant EGFR inhibitor suppresses FGFR WT with an IC50 of 0.4 nM. NT-1 also inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M. NT-1 exerts deeper inhibition on p-EGFR and p-ERK, and induces tumor cell apoptosis. NT-1 can be used in colorectal cancer research .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
