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Tizaterkib

(Synonyms: AZD0364)

目录号: PL01919 纯度: ≥99%

Tizaterkib (AZD0364) 是一种有效的选择性 ERK2 抑制剂，IC50 为 0.6 nM。详细信息请参考专利文献 WO2017080979A1 中的化合物 example 18。

CAS No. :2097416-76-5

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中文名称	Tizaterkib
英文名称	Tizaterkib
英文别名	AZD0364;Q50825500;(6~{R})-7-[[3,4-bis(fluoranyl)phenyl]methyl]-6-(methoxymethyl)-2-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-5,6-dihydroimidazo[1,2-a]pyrazin-8-one;(6R)-7-(3,4-Difluorobenzyl)-6-(methoxymethyl)-2-{5-methyl-2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl}-6,7-dihydroimidazo[1,2-a]pyrazin-8(5H)-one;(R)-7-(3,4-difluorobenzyl)-6-(methoxymethyl)-2-(5-methyl-2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)-;(R)-7-(3,4-Difluorobenzyl)-6-(methoxymethyl)-2-(5-methyl-2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidi;AZD-0364;Tizaterkib
Cas No.	2097416-76-5
分子式	C₂₄H₂₄F₂N₈O₂
分子量	494.50
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	Tizaterkib (AZD0364) 是一种有效的选择性 ERK2 抑制剂，IC50 为 0.6 nM。详细信息请参考专利文献 WO2017080979A1 中的化合物 example 18。

产品详情	Tizaterkib (AZD0364) 是一种有效的选择性 ERK2 抑制剂，IC₅₀ 为 0.6 nM。详细信息请参考专利文献 WO2017080979A1 中的化合物 example 18。
生物活性	Tizaterkib (AZD0364) is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC 50 of 0.6 nM.
性状	Solid
IC50 & Target[1][2]	ERK2 0.6 nM (IC50)
体外研究(In Vitro)	Tizaterkib is measured in the ERK2 mass spectrometry and A375 phospho-p90RSK assays with IC50s of 0.6 nM and 5.7 nM, respectively. Tizaterkib can inhibit the growth of a panel of cancer cell lines (A549, H2122, H2009, and Calu6 cell lines) with KRAS mutations as a monotherapy and this effect is synergistically enhanced by treatment with Selumetinib. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Tumor growth inhibition by Tizaterkib ethanesulfonic acid (Example 18a) in combination with MEK inhibitor Selumetinib is measured. Studies are performed in the A549 xenograft model. Selumetinib is dosed twice daily (BiD) 8 hours apart and Tizaterkib ethanesulfonic acid is dosed once daily (QD) 4 hours after the first Selumetinib dose. Both compounds are dosed continuously for 3 weeks. Both vehicles are dosed in the vehicle group. Both Selumetinib and Tizaterkib ethanesulfonic acid reduce tumor growth relative to vehicle only control. The combination of Selumetinib and Tizaterkib ethanesulfonic acid results in a reduction in tumor growth. 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]. WARD, Richard, Andrew, et al. DIHYDROIMIDAZOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER. WO2017080979A1.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (202.22 mM)配制储备液

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[1]. WARD, Richard, Andrew, et al. DIHYDROIMIDAZOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER. WO2017080979A1.

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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