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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
53 Results for "
lung permeability
" in MedChemExpress (MCE) Product Catalog:
Products (53)
53 Results for "lung permeability" in MCE Product Catalog:
4
4 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 .
4
4 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 .
4
4 Cited Publications
Cat. No.: HY-W424851
CAS No.: 84050-22-6
Synonyms: 6,7-Dimethoxy-2-(1-piperazinyl)-4-quinazolinamine hydrochloride
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DPQ hydrochloride is a blood-brain barrier permeable and selective PARP-1 inhibitor that blocks PARP-1-mediated DNA damage repair and NAD +/ATP consumption, thereby inhibiting excessive inflammatory responses. DPQ hydrochloride inhibits NF-κB pathway activation, reduces the expression of pro-inflammatory factors (such as TNF-α, IL-6) and oxidative stress. DPQ hydrochloride can be used in inflammation-related studies of acute lung injury, myocardial infarction, and neurodegenerative diseases .
3
3 Cited Publications
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BOS-318 is a potent, slowly dissociating, highly selective, and cell-permeable furin inhibitor with IC50 value of 1.9 nM. BOS-318 protects ENaC from subsequent activation by neutrophil elastase. BOS-318 can be used for the rsearch for CF lung disease .
1
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Patritumab deruxtecan (HER3-DXd) is an antibody-drug conjugate (ADC) targeting HER3, consisting of the anti-HER3 IgG1 antibody Patritumab (HY-P99275), a cleavable tetrapeptide linker, and the membrane-permeable topoisomerase I (Topoisomerase Ⅰ) inhibitor DXd (HY-13631D). After binding to membrane-localized HER3, Patritumab deruxtecan is internalized into lysosomes, where the linker is cleaved to release DXd. DXd enters the nucleus to induce DNA damage and cell death, and exerts a bystander effect via transmembrane diffusion. Patritumab deruxtecan reduces the viability of HER3-positive cells and induces features of immunogenic cell death including CALR membrane exposure, ATP and HMGB1 release, and can be used in studies related to HER3-positive breast cancer and non-small cell lung cancer .
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1
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Carbinoxamine maleate salt is a blood-brain barrier-permeable histamine H1 receptor antagonist. Carbinoxamine maleate salt blocks the action of histamine on H1 receptors, reducing symptoms such as sneezing, rhinitis, rhinorrhea, erythema, pruritus and urticaria. Carbinoxamine maleate salt inhibits influenza virus entry into cells via endocytosis, targets the early stage of the viral life cycle, and simultaneously reduces viral replication levels in the lungs, alleviating pathological damage and inflammatory responses in lung tissues. Carbinoxamine maleate salt can be used in research on allergic rhinitis, influenza, etc.
1
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BAMB-4 (ITPKA-IN-C14) is a specific and membrane-permeable ITPKA inhibitor. BAMB-4 has high stability and membrane permeability and against the inositol-1,4,5-trisphosphate (InsP3) kinase activity of inositol-1,4,5-trisphosphate-3-kinase A (ITPKA) with an IC50 value of 20 μM. BAMB-4 can be used for the research of metastasis of lung cancer .
1
1 Cited Publications
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YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM. YUKA1 has less inhibitory active on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 can increase H3K4me3 levels and inhibit cell proliferation. YUKA1 can be used for the research of cancer, such as lung and breast cancers .
1
1 Cited Publications
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Semustine is an orally active, blood-brain barrier permeable antitumor alkylating agent with a binding affinity of 1.53 × 10 3 M -1 for guanine and thymine residues in bovine DNA. Semustine undergoes major groove-directed alkylation at guanine residues to form O6-chloroethylguanine and N1-O6-ethanoguanine adducts, and generates dG-dC interstrand crosslinks. Semustine induces partial B- to C-type transition of DNA, base stacking and helical structure distortion, mild dehydration, as well as partial DNA double-strand unwinding. Semustine can be used in research related to Lewis lung cancer, leukemia, Hodgkin's lymphoma, malignant melanoma, glioma, and diffuse large B-cell lymphoma .
1
1 Cited Publications
Cat. No.: HY-N7694
CAS No.: 97871-44-8
Category:
Triterpenes Plant Terpenoids Meliaceae Extract Melia toosendan Sieb. et Zucc. Extract Disease Research Fields Inflammation/Immunology
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1
1 Cited Publications
Cat. No.: HY-117720A
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OSU-2S TFA is a non-immunosuppressive derivative of Fingolimod hydrochloride (FTY720) (HY-12005). It is an orally active, blood-brain barrier-permeable allosteric activator of PP2A that also activates PKCδ; it restores PP2A activity by displacing the inhibitory protein SET, thereby inducing ROS-PKCδ-caspase-3-dependent apoptosis, c-Myc degradation, cell cycle arrest, and differentiation. OSU-2S TFA is used in research on diseases such as leukemia, liver cancer, lymphoma, and lung cancer .
Cat. No.: HY-173629
CAS No.: 3082166-76-2
RMC-5127 is a small molecule inhibitor that binds to GTP-targeted KRAS G12V, with oral bioavailability and blood-brain barrier permeability. RMC-5127 inhibits the activities of the RAS and MAPK pathways, suppresses the proliferation of KRAS G12V-mutant cancer cells and induces their apoptosis. RMC-5127 can be used for the research of KRAS G12V-mutant non-small cell lung cancer, pancreatic ductal adenocarcinoma, colorectal cancer and intracranial KRAS G12V tumors .
Synonyms: SHR169265
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(αR)-Cyclopropaneacetamide-Exatecan (SHR169265) is a DNA Topoisomerase I inhibitor with enhanced membrane permeability (with an IC50 of 1.34 μM against the human DNA Topoisomerase I). (αR)-Cyclopropaneacetamide-Exatecan exerts cytotoxic effects by inhibiting the enzymatic activity of Topoisomerase I, and this anticancer effect is independent of the expression level of HER2. (αR)-Cyclopropaneacetamide-Exatecan is an ADC Cytotoxin derived from Exatecan (HY-13631), which can be used in research related to advanced cancers such as breast cancer, gastric cancer, colorectal cancer and non-small cell lung cancer .
Cat. No.: HY-19763
CAS No.: 1235449-52-1
Synonyms: BEBT-908
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Ifupinostat (BEBT-908) is a blood-brain barrier-permeable PI3K/HDAC inhibitor. Ifupinostat exerts anticancer activity against hematologic malignancies, lung cancer, colon cancer, brain cancer and other cancers. Ifupinostat inhibits the PI3K/AKT/mTOR signaling pathway, suppresses c-Myc expression and induces ferroptosis. Ifupinostat can be used in tumor research .
Synonyms: Brigatinib analog
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ALK-IN-1 is an orally active, blood-brain barrier-permeable ALK and EGFR inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer .
Cat. No.: HY-N0660
CAS No.: 55466-05-2
Cat. No.: HY-139300
CAS No.: 1203902-67-3
Synonyms: HMPL-813
Epitinib (HMPL-813) is a selective, orally active, blood-brain barrier-permeable EGFR tyrosine kinase inhibitor. Epitinib is applicable to research on EGFR T790M-positive non-small cell lung cancer with brain metastasis and advanced solid tumors .
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BRL-44408 maleate is a selective, blood-brain barrier-permeable α2A-adrenergic receptor antagonist with a Ki value of 8.56 nM against human targets. BRL-44408 maleate exhibits activities such as antidepressant, analgesic effects and attenuation of sepsis-induced acute lung injury by regulating the release of neurotransmitters such as norepinephrine and dopamine, or inhibiting signaling pathways including ERK1/2, p38MAPK and p65. BRL-44408 maleate can be used in studies related to acute respiratory distress syndrome, depression and visceral pain .
Cat. No.: HY-P10580
CAS No.: 1359657-45-6
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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
