GW779439X|551919-98-3|-陌孚医药/Medlife

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GW779439X

目录号: PL13935 纯度: ≥99%

CAS No. :551919-98-3

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中文名称	GW779439X
中文别名	N-[4-(4-甲基-1-哌嗪基)-3-(三氟甲基)苯基]-4-(吡唑并[1,5-b]哒嗪-3-基)-2-嘧啶胺;化合物GW779439X
英文名称	GW779439X
英文别名	GW779439X;N-[4-(4-methylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine;C22H26Cl2N2O6;AOB4343;SYN5179;HMS3303B12;HMS3305K24;BDBM50293150;NSC756341;N-(4-(4-methylpiperazin-1-yl)-3-;J3.496.857H;A900422;(trifluoromethyl)phenyl)-4-(pyrazolo[1,5-b]pyridazin-3-yl) pyrimidin-2-amine;N-(4;2-Pyrimidinamine, N-[4-(4-methyl-1-piperazinyl)-3-(trifluoromethyl)phenyl]-4-pyrazolo[1,5-b]pyridazin-3-yl-
Cas No.	551919-98-3
分子式	C₂₂H₂₁F₃N₈
分子量	454.45
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	GW779439X，吡唑并吡啶类化合物，是一种金黄色葡萄球菌 PASTA 激酶 Stk1 抑制剂。GW779439X 增强 β-内酰胺类抗生素对各种 MRSA 和 MSSA 的分离株，有的甚至跨越了从耐药到敏感的断点。GW779439X 是一种 AURKA 抑制剂，可通过 caspases 3/7 诱导细胞凋亡 (apoptosis)。
生物活性	GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway. MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
性状	Solid
IC50 & Target[1][2]	Aurora A Stk1
体外研究(In Vitro)	GW779439X (2 μM) biochemically inhibits Stk1. GW779439X (5 μM) potentiates ceftaroline activity against a ceftaroline-resistant MRSA strain. GW779439X is able to potentiate the activity of oxacillin against various S. aureus isolates, including both MRSA and MSSA isolates, but the potentiation is clearly strongest in PBP2A-containing strains. GW779439X has growth inhibition effects on the AGP-01 cell line (IC50= 0.57 μM). GW779439X (1μM) significantly blockS the cell cycle at the G0/G1 phase and sub-G1 phase. GW779439X (1μM; 72 hours; AGP-01 cells) significantly decreases expression levels of genes involved in proliferation progression ( c-MYC , NRAS , and CDC25A ) and increases expression levels of genes involved in cell cycle blocking ( CDKN1A and TP53 ).
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Mesquita FP, et al. Kinase inhibitor screening reveals aurora-a kinase is a potential therapeutic and prognostic biomarker of gastric cancer [published online ahead of print, 2021 Jun 23]. J Cell Biochem. 2021;10.1002/jcb.30015. [2]. Schaenzer AJ, et al. GW779439X and Its Pyrazolopyridazine Derivatives Inhibit the Serine/Threonine Kinase Stk1 and Act As Antibiotic Adjuvants against β-Lactam-Resistant Staphylococcus aureus. ACS Infect Dis. 2018;4(10):1508-1518.

溶解度数据	In Vitro: DMSO : 31.25 mg/mL (68.76 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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