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| | N-[4-メチル-3-(3-メチル-4-オキソ-3,4-ジヒドロキナゾリン-6-イルアミノ)フェニル]-3-(1-シアノ-1-メチルエチル)ベンズアミド 製品概要 |
| 化学名: | N-[4-メチル-3-(3-メチル-4-オキソ-3,4-ジヒドロキナゾリン-6-イルアミノ)フェニル]-3-(1-シアノ-1-メチルエチル)ベンズアミド | | 英語化学名: | AZ 628 | | 别名: | 3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]benzamide;AZ-628;AZ628/AZ-628;AZD628;3-(2-cyanopropan-2-yl)-N-(4-methyl-3-(3-methyl-4-oxo-3,4-dihydroquinazolin-6-ylamino)phenyl)benzamide;AZ628, >=99%;3-(2-Cyanopropan-2-yl)-N-(4-methyl-3-((3-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino)phenyl)ben;Benzamide, 3-(1-cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]- | | CAS番号: | 878739-06-1 | | 分子式: | C27H25N5O2 | | 分子量: | 451.52 | | EINECS: | | | カテゴリ情報: | Inhibitors;MAPK | | Mol File: | 878739-06-1.mol | ![N-[4-メチル-3-(3-メチル-4-オキソ-3,4-ジヒドロキナゾリン-6-イルアミノ)フェニル]-3-(1-シアノ-1-メチルエチル)ベンズアミド](CAS2/GIF/878739-06-1.gif) |
| | N-[4-メチル-3-(3-メチル-4-オキソ-3,4-ジヒドロキナゾリン-6-イルアミノ)フェニル]-3-(1-シアノ-1-メチルエチル)ベンズアミド 物理性質 |
| 比重(密度) | 1.21±0.1 g/cm3(Predicted) | | 貯蔵温度 | -20°C | | 溶解性 | DMSO: soluble10mg/mL, clear | | 外見 | powder | | 酸解離定数(Pka) | 12.92±0.70(Predicted) | | 色 | white to beige |
| | N-[4-メチル-3-(3-メチル-4-オキソ-3,4-ジヒドロキナゾリン-6-イルアミノ)フェニル]-3-(1-シアノ-1-メチルエチル)ベンズアミド Usage And Synthesis |
| 使用 | AZ 628 is an inhibitor of B-RAF and B-RAF(V600E) | | 定義 | ChEBI: 3-(2-cyanopropan-2-yl)-N-[4-methyl-3-[(3-methyl-4-oxo-6-quinazolinyl)amino]phenyl]benzamide is a member of benzamides. | | 生物活性 | az628 is a potent and newly discorvered inhibitor of braf, c-raf-1 and brafv600e with ic50 values of 105 nm, 29 nm and 34 nm, respectively. this compound prevents craf activation through persistently occupying the atp-binding site of raf kinase. specificity profile suggests that az628 also inhibits activation of other tyrosine protein kinases such as ddr2, vegfr2, lyn, flt1, fms and others.raf kinases a family of three serine/threonine-specific protein kinases and participate in the ras-raf-mek-erk signal transduction cascade, also known as the mitogen-activated protein kinase (mapk) cascade. the activation of mapk signaling leads to different cellular response such as cell proliferation, apoptosis and inflammation.az628 has the potent anti-tumor activity. in human colon and melanoma-derived cell line that carries the recurrent v600e activating braf mutation, az628 was shown to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis [1]. az628 may be antiangiogenic due to inhibition of vegfr2 [2].generation of melanoma cell line clones is obtained resistance to the raf kinase inhibitor az628. resistance to az628 is connected with raised levels of the raf downstream effector p-erk1/2. erk1/2 initiation in az628-resistant clones is interceded by mek. supported multiplication of az628-resistant clones is to a great extent autonomous of braf kinase action. az628-resistant clones express elevated craf. survival of az628-safe cells is subject to craf [1]. | | in vitro | AZ628 inhibits B-Raf, B-Raf AZ628 acts on B-Raf-containing M14 parental cell lines treated with increasing concentrations of AZ628, an effective inhibition of p-ERK1/2 levels was observed. It acts on AZ628-resistant M14 cells and does not inhibit ERK activation. AZ628 acts on NRAS-mutated malignant melanoma cells and effectively reduces ERK activation. | | target | | Target | Value | C-Raf-1
(Cell-free assay) | 29 nM | B-Raf (V600E)
(Cell-free assay) | 34 nM | B-Raf
(Cell-free assay) | 105 nM |
| | 貯蔵 | Store at +4°C | | 参考文献 | 1. montagut c, sharma sv, shioda t, mcdermott u, ulman m, ulkus le, et al. elevated craf as a potential mechanism of acquired resistance to braf inhibition in melanoma. cancer res 2008,68:4853-4861.2. khazak v, astsaturov i, serebriiskii ig, golemis ea. selective raf inhibition in cancer therapy. expert opin ther targets 2007,11:1587-1609. |
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