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Aromatic organic compounds that consist of a phenyl functional group (−C6H5) bonded to a hydroxyl functional group (−OH). Includes all compounds that do not have additional substitutions.
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AG-490 is an inhibitor of EGFR with IC50 of 0 1 M in cell-free assays 135-fold more selective for EGFR versus ErbB2 also inhibits JAK2 with no activity to Lck Lyn Btk Syk and Src
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AG-14361 (CAS 328543-09-5) is a highly selective inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1) exhibiting a Ki50 of less than 5 nM PARP-1 is integral to DNA repair and cell death pathways and is overexpressed in various tumor types AG-14361 has demonstrated the ability to sensitize homologous recombination (HR) and BRCA2-deficient cells to DNA-damaging agents at non-cytotoxic concentrations In human K562 cells AG-14361 enhances camptothecin-induced growth inhibition and cytotoxicity while increasing DNA single-strand breaks It also restores temozolomide sensitivity in mismatch repair-proficient cells Preclinical models indicate greater antitumor responses in BRCA2-deficient xenografts following AG-14361 administration supporting its use in DNA repair and cancer research
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Specific inhibitor of insulin-like growth factor-1 (IGF-1) and insulin receptor kinases. Induces apoptosis by downregulation of the expression of phospho-Akt1 and Bcl-2. Also increases Bax, p53 and p21 expression. Formula: C14H13BrN2O. MW: 305.2. Purity: ≥98% (HPLC (UV)). Solubility: Soluble in acetonitrile (5mg/ml), DMSO (8mg/ml), dichloromethane (23mg/ml) or methanol (5mg/ml); insoluble in 100% ethanol. Long Term Storage: -20°C.
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PDGF inhibitor. Selective inhibitor of tyrosine kinase in platelet-derived growth factor (PDGF) receptor. Alternative name: 6,7-Dimethyl-2-phenylquinoxaline. Formula: C16H14N2. MW: 234.3. Purity: ≥98% (HPLC). Solubility: Soluble in DMSO. Long Term Storage: -20°C. Handling: Store tightly sealed in the dark. Protect from light.
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Alternative name: Tyrphostin B44, (-)-(R)-N-(alpha-Methylbenzyl)-3,4-dihydroxybenzylidenecyanoacetamide. Formula: C18H16N2O3. MW: 308.3. Purity: ≥98% (HPLC). Solubility: Soluble in DMSO or 100% ethanol. Long Term Storage: -20°C. Handling: Store tightly sealed in the dark. Protect from light.
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Specific inhibitor of insulin-like growth factor-1 (IGF-1) and insulin receptor kinases. Induces apoptosis by downregulation of the expression of phospho-Akt1 and Bcl-2. Also increases Bax, p53 and p21 expression. Formula: C14H13BrN2O. MW: 305.2. Purity: ≥98% (HPLC (UV)). Solubility: Soluble in acetonitrile (5mg/ml), DMSO (8mg/ml), dichloromethane (23mg/ml) or methanol (5mg/ml); insoluble in 100% ethanol. Use/Stability: In a dissolved form it should be stable for at least 1 month. Long Term Storage: -20°C. Handling: Protect from light.
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This compound is a tyrosine kinase inhibitor that specifically acts on TrKA phosphorylation and also functions as a selective ErbB2 tyrosine kinase inhibitor. It demonstrates significantly higher selectivity for ErbB2 compared to EGFR. This agent exhibits anticancer properties by reducing cell proliferation and inducing apoptosis in various cell lines, and has shown to decrease tumor growth in animal models.
Inhibits TrKA phosphorylation.
Selective ErbB2 tyrosine kinase inhibitor.
Exhibits at least 500-fold higher selectivity to ErbB2 than EGFR.
Possesses anticancer activity.
Decreases cell proliferation in various cell lines.
Induces apoptosis in multiple cell lines.
Reduces tumor growth in athymic, immunodepressed mice.
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