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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
19 Results for "
EGFR enzyme
" in MedChemExpress (MCE) Product Catalog:
Products (19)
19 Results for "EGFR enzyme" in MCE Product Catalog:
1
1 Cited Publications
Cat. No.: HY-48999A
CAS No.: 3033987-42-4
FSK hydrochloride is fluorosulfonyloxybenzoyl-L-lysine, which features a long, flexible aryl fluorosulfate-containing side chain that can reach protein sites inaccessible to covalent conjugation. FSK hydrochloride modifies nanomolecules to target epidermal growth factor receptor (EGFR), resulting in irreversibly bound covalent interactions. Through genetically encoded chemical crosslinking, FSK hydrochloride captures unknown enzyme-substrate interactions in living cells, targets residues other than Cys, and mediates crosslinking at the binding periphery. FSK hydrochloride enables the construction of a bioreactive SuFEx system for generating covalent bonds in various proteins both in vitro and in vivo .
1
1 Cited Publications
Cat. No.: HY-N12445
CAS No.: 19254-30-9
Target:
Target:
Research Areas:
LM2I is a derivative of Spinosyn A (SPA). LM2I is argininosuccinate synthase (ASS1) enzyme activator, and tumor inhibitor that directly interact with ASS1. LM2I has significant antiproliferative activity in seven colorectal cancer cell-lines and xenograft tumors of colorectal cancer. LM2I inhibits colorectal cancer cell growth via the EGFR pathway .
Synonyms: Mifanertinib
Mefatinib free base (Mifanertinib) is an orally active EGFR and HER2 kinase inhibitor with IC50 values of 0.4 nM and 11.7 nM, respectively. Mefatinib free base inhibits tumor growth in mouse models of lung cancer xenografts that overexpress EGFR/HER2, carry EGFR mutations, or carry Erlotinib (HY-50896)-resistant EGFR double mutations. Mefatinib free base can be used for the research of advanced EGFR-mutant non-small cell lung cancer .
Category:
Cardiovascular Disease Alkaloids other families Phenols Polyphenols Plants Disease Research Fields Isoquinoline Alkaloids
Target:
Cat. No.: HY-N9454
CAS No.: 91893-83-3
Cat. No.: HY-178955
EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer .
Cat. No.: HY-178448
Target:
EGFR JAK Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Cannabinoid Receptor Glutathione Peroxidase Caspase
Research Areas:
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) .
Cat. No.: HY-149636
Purity: 99.82%
Multi-target kinase inhibitor 2 is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values of 79 nM, 40 nM,136 nM, and 204 nM, respectively. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells .
Cat. No.: HY-156470
CAS No.: 3009081-73-3
Target:
Trk Receptor Anaplastic lymphoma kinase (ALK) c-Kit EGFR Pim Casein Kinase Checkpoint Kinase (Chk) CDK Apoptosis
Research Areas:
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
Synonyms: Mifanertinib dimaleate
Mefatinib (Mifanertinib dimaleate) is an orally active EGFR and HER2 kinase inhibitor with IC50 values of 0.4 nM and 11.7 nM, respectively. Mefatinib inhibits tumor growth in mouse models of lung cancer xenografts that overexpress EGFR/HER2, carry EGFR mutations, or carry Erlotinib (HY-50896)-resistant EGFR double mutations. Mefatinib can be used for the research of advanced EGFR-mutant non-small cell lung cancer .
Cat. No.: HY-158154
CAS No.: 3061531-76-5
EGFR-IN-110 (Compound 6) is a covalent EGFR inhibitor, with pIC50 values of 9.2 and 8.7 for EGFR enzyme and EGFR cell, respectively. EGFR-IN-110 shows high EGFR potency and good kinase selectivity .
Cat. No.: HY-158177
CAS No.: 3032760-71-4
EGFR T790M/L858R-IN-6 (compound 53), a pyrimidine compound, is a potent EGFR T790M/L858R inhibitor. EGFR T790M/L858R-IN-6 shows 90.88% enzyme activity inhibition with 0.05 μM .
Category:
Cardiovascular Disease Alkaloids Phenols Polyphenols Nelumbo nucifera Gaertn. Plants Disease Research Fields Isoquinoline Alkaloids Nymphaeaceae
Target:
Cat. No.: HY-152852S
Synonyms: Mifanertinib-d6
Cat. No.: HY-179529
EGFR/InhA-IN-1 (Compound 15) is an inhibitor of the anti-cancer target EGFR tyrosine kinase (1M17) (Ki = 0.05 μM) and the anti-tuberculosis target InhA enzyme (1OUZ) (Ki = 0.02 μM). EGFR/InhA-IN-1 exhibits anti-proliferative activity against A549 cells, with an IC50 of 10.38 μM. EGFR/InhA-IN-1 has inhibitory activity against Mycobacterium tuberculosis H37Rv, with a MIC of 6.25 μM. EGFR/InhA-IN-1 can be used for research on non-small cell lung cancer and Mycobacterium tuberculosis infection .
Cat. No.: HY-L009
3,970 compounds
Kinase is an enzyme that adds phosphate groups to other molecules. This process is known as phosphorylation. Protein phosphorylation is a key aspect in the regulation of a large number of cellular processes including cellular division, metabolism, signal transduction, and so on. There are over 500 kinases encoded by the human genome and it has been estimated that kinases regulate approximately 50% of cellular functions. Kinases are a large group of drug targets in drug discovery. Kinase inhibitors are an important class of drugs that block certain enzymes involved in diseases such as cancer and inflammatory disorders.
Kinase inhibitor library designed by MCE contains 3,970 kinase inhibitors and regulators mainly targeting protein kinases (VEGFR, EGFR, BTK, CDK, Akt, etc.), lipid kinases (PI3K, PI4K, SK, etc.) and carbohydrate kinases (Hexokinase), and is a useful tool for kinase drug discovery and related research.
Cat. No.: HY-L009M
271 compounds
Kinases is a class of enzymes that adds chemicals called phosphates to other molecules, such as sugars or proteins. Protein phosphorylation serves as a critical regulatory mechanism for numerous cellular processes including cell division, metabolism, and signal transduction, with approximately 50% of cellular functions in humans being regulated by kinase activity. In drug discovery, kinases represent a major category of therapeutic targets, and kinase inhibitors constitute an important class of pharmaceuticals that block the activity of specific disease-associated enzymes, particularly in cancer and inflammatory disorders. Small molecule kinase inhibitors represent one of the fastest-growing drug categories, having received U.S. Food and Drug Administration (FDA) approval for both oncological and non-oncological indications. As of September 2023, over 70 FDA-approved small molecule kinase inhibitors are commercially available.
The MCE Kinase Inhibitor Library Mini contains 271 kinase inhibitors primarily targeting protein kinases (VEGFR, EGFR, BTK, CDK, Akt, etc.), lipid kinases (PI3K, PI4K, SK, etc.), and carbohydrate kinases. This collection includes 1-3 highly specific representative compounds per target, optimized for screening of kinase-related drug targets in pharmaceutical 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
