化合物MLN2480 T6895
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Product IntroductionBioactivity英文名: TAK-580描述: TAK-580 (MLN2480) 是一种可口服的选择性Raf 广谱抑制剂。动物实验: [4]Animal Models: C57BL/6J mic
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Product Introduction
Bioactivity
英文名: TAK-580
描述: TAK-580 (MLN2480) 是一种可口服的选择性Raf 广谱抑制剂。
动物实验: [4]Animal Models: C57BL/6J miceFormulation: 100% PEG400Dosages: 12.5 mg/kgAdministration: oral gavage
体外活性: MLN2480 inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preClinicalal cancer models at concentrations that are tolerated in vivo. It is found to activate phosphorylated MEK at very low concentrations, but inhibits this same activity at higher concentrations. The inhibitory effects of MLN-2480 are found to vary across models and genetic contexts. In vitro analysis of this drug combination of MLN2480 and TAK-733(an investigational allosteric MEK kinase inhibitor) in cell proliferation assays demonstrates synergistic activity. In addition, western blot analysis demonstrates the effect of MLN2480 in reversing feedback activation of MEK in response to TAK-733, leading to more concerted MAPK pathway inhibition.MLN-2480 only modestly inhibits PRAK.
体内活性: In vivo, MLN2480 shows antitumor activity in melanoma, colon, lung, and pancreatic cancer xenograft models.MLN-2480 (37.5 mg/kg) is well tolerated in a tumor xenograft model. The combination of MLN-2480 (12.5 mg) and TAK-733 (1 mg/kg) is effective in an SK-MEL-30 xenograft model, but monotherapy with either compound produces negligible effects.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (183.7 mM)
Ethanol : 93 mg/mL (183.7 mM)
关键字: MLN 2480 | BIIB 024 | Raf kinases | inhibit | MLN-2480 | TAK 580 | Raf | BIIB024 | Inhibitor | TAK580 | TAK-580
相关产品: Rineterkib | LY2452473 | GSK1904529A | Uplarafenib | PROTAC B-Raf degrader 1 | Dabrafenib Mesylate | Sorafenib tosylate | AZ304 | Sulindac sulfide | MCP110
相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | Orally Active Compound Library
Bioactivity
英文名: TAK-580
描述: TAK-580 (MLN2480) 是一种可口服的选择性Raf 广谱抑制剂。
动物实验: [4]Animal Models: C57BL/6J miceFormulation: 100% PEG400Dosages: 12.5 mg/kgAdministration: oral gavage
体外活性: MLN2480 inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preClinicalal cancer models at concentrations that are tolerated in vivo. It is found to activate phosphorylated MEK at very low concentrations, but inhibits this same activity at higher concentrations. The inhibitory effects of MLN-2480 are found to vary across models and genetic contexts. In vitro analysis of this drug combination of MLN2480 and TAK-733(an investigational allosteric MEK kinase inhibitor) in cell proliferation assays demonstrates synergistic activity. In addition, western blot analysis demonstrates the effect of MLN2480 in reversing feedback activation of MEK in response to TAK-733, leading to more concerted MAPK pathway inhibition.MLN-2480 only modestly inhibits PRAK.
体内活性: In vivo, MLN2480 shows antitumor activity in melanoma, colon, lung, and pancreatic cancer xenograft models.MLN-2480 (37.5 mg/kg) is well tolerated in a tumor xenograft model. The combination of MLN-2480 (12.5 mg) and TAK-733 (1 mg/kg) is effective in an SK-MEL-30 xenograft model, but monotherapy with either compound produces negligible effects.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (183.7 mM)
Ethanol : 93 mg/mL (183.7 mM)
关键字: MLN 2480 | BIIB 024 | Raf kinases | inhibit | MLN-2480 | TAK 580 | Raf | BIIB024 | Inhibitor | TAK580 | TAK-580
相关产品: Rineterkib | LY2452473 | GSK1904529A | Uplarafenib | PROTAC B-Raf degrader 1 | Dabrafenib Mesylate | Sorafenib tosylate | AZ304 | Sulindac sulfide | MCP110
相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | Orally Active Compound Library
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