A 419259 trihydrochloride|1435934-25-0|(RK 20449 trihydrochloride)-陌孚医药/Medlife

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A 419259 trihydrochloride (Synonyms: RK 20449 trihydrochloride)

目录号: PC16090 纯度: ≥98%

CAS No. :1435934-25-0

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中文名称	A 419259 trihydrochloride
中文别名	7-[反式-4-(4-甲基-1-哌嗪基)环己基]-5-(4-苯氧基苯基)-7H-吡咯并[2,3-D]嘧啶-4-胺三盐酸盐;A 419259 (trihydrochloride)
英文名称	A 419259 trihydrochloride
英文别名	7-[trans-4-(4-Methyl-1-piperazinyl)cyclohexyl]-5-(4-phenoxyphenyl )-7H-pyrrolo[2,3-d]pyrimidin-4-amine trihydrochloride;A 419259 trihydrochloride;A-419259 trihydrochloride;RK 20449 trihydrochloride;RK-20449 trihydrochloride;A 419259 (trihydrochloride)
Cas No.	1435934-25-0
分子式	C₂₉H₃₇Cl₃N₆O
分子量	592.00
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性	A 419259 trihydrochloride is a Src family kinases inhibitor with IC₅₀s of 9 nM, 3 nM and 3 nM for Src, Lck and Lyn, respectively.
性状	Solid
IC50 & Target[1][2]	IC50: 9 nM (Src), <3 nM (Lck), <3 nM (Lyn), 3 μM (Abl)
体外研究(In Vitro)	A 419259 Trihydrochloride is a second-generation pyrrolo-pyrimidine designed to enhance selectivity towards the Src family relative to other cytoplasmic tyrosine kinases. A-419259 inhibits K-562 cells with an IC₅₀ between 0.1 and 0.3 μM, and Meg-01 proliferation with an IC₅₀ of approximately 0.1 μM. A-419259 also potently induces apoptosis in K-562 cells beginning at 0.1 μM and increasing in a dose-dependent manner. PP2 inhibits Src kinase autophosphorylation in both Ph cell lines (K-562 and Meg-01) with an IC₅₀ between 3 and 10 μM, while A-419259 blocks kinase activation between 0.1 and 0.3 μM. A-419259 strongly inhibits DAGM/Bcr-Abl cell proliferation in the absence of IL-3 with an IC₅₀ between 0.1 and 0.3 μM. A-419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, and blocks proliferation and induces apoptosis in CML cell lines. A-419259 inhibits overall SFK activity in K562 and other CML cell lines with an IC₅₀ value of 0.1-0.3 μM. Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature or refrigerated transportation.
储存方式	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Wilson MB, et al. Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr-Abl signal transduction and oncogenesis. Oncogene. 2002 Nov 21;21(53):8075-88. [Information] [2]. Pene-Dumitrescu T, et al. An inhibitor-resistant mutant of Hck protects CML cells against the antiproliferative and apoptotic effects of the broad-spectrum Src family kinase inhibitor A-419259.Oncogene (2008) 27, 7055-7069 [Information]

溶解度数据

体外研究:

H₂O : ≥ 55 mg/mL (92.91 mM)

DMSO : 1 mg/mL (1.69 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6892 mL	8.4459 mL	16.8919 mL
5 mM	0.3378 mL	1.6892 mL	3.3784 mL
10 mM	0.1689 mL	0.8446 mL	1.6892 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (168.92 mM); Clear solution; Need ultrasonic

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产品使用指南

Data Sheet

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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