XMD17-109|1435488-37-1|-陌孚医药/Medlife

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XMD17-109

目录号: PL04494 纯度: ≥99%

CAS No. :1435488-37-1

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中文名称	XMD17-109
中文别名	11-环戊基-2-[[2-乙氧基-4-[[4-(4-甲基-1-哌嗪基)-1-哌啶基]羰基]苯基]氨基]-5,11-二氢-5-甲基-6H-嘧啶并[4,5-B][1,4]苯并二氮杂卓-6-酮;XMD17-109 抑制剂
英文名称	XMD17-109
英文别名	XMD17-109;11-cyclopentyl-2-[[2-ethoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dihydro-5-methyl-6H-Pyrimido[4,5-b][1,4]benzodiazepin-6-one;11-cyclopentyl-2-[2-ethoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5-methylpyrimido[4,5-b][1,4]benzodiazepin-6-one;ERK5-IN-1;XMD17 109;11-Cyclopentyl-2-((2-ethoxy-4-(4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl)-phenyl)amino)-5-methyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
Cas No.	1435488-37-1
分子式	C₃₆H₄₆N₈O₃
分子量	638.80
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	XMD17-109 是一种特异性的 ERK-5 抑制剂，IC₅₀ 值为 162 nM。
生物活性	XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC 50 of 162 nM.
性状	Solid
IC50 & Target[1][2]	ERK5 162 nM (IC50) LRRK2[G2019S] 339 nM (I
体外研究(In Vitro)	XMD17-109 (Compound 26) inhibits ERK5 biochemically with an IC50 of 0.162 ± 0.006 μM, and blocks pidermal growth factor induced ERK5 autophosphorylation with an EC50 of 0.09 ± 0.03 μM in cells. XMD17-109 also inhibits LRRK2[G2019S] with an IC50 of 339 nM. XMD17-109 demonstrats low nanomolar cellular activity judged by the significant dose-dependent reduction of mobility shifted phosphorylated ERK5 bands from sorbitol stimulated cells. XMD17-109 completely inhibits the ERK5-mediated AP1 transcriptional activity at 30 μM and has an EC50 of 4.2 μM. has not independently confirmed the accuracy of these methods. They are for reference only.
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]. Deng X, et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem. 2013;70:758-67. [2]. Elkins, Jonathan M., et al. X-ray Crystal Structure of ERK5 (MAPK7) in Complex with a Specific Inhibitor. Journal of Medicinal Chemistry (2013), 56(11), 4413-4421.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (156.54 mM)配制储备液

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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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