AT7519 Hydrochloride|902135-91-5|-陌孚医药/Medlife

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AT7519 Hydrochloride

目录号: PL05101 纯度: ≥99%

CAS No. :902135-91-5

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中文名称	AT7519 Hydrochloride
中文别名	N-(4-哌啶基)-4-(2,6-二氯苯甲酰基氨基)-1H-吡唑-3-甲酰胺盐酸盐;Boc-(3S,4S,5S)-4-氨基-3-羟基-5-甲基庚酸二环己基铵盐;N-(4-哌啶基)-4-(2,6-二氯苄氨基)-1H-吡唑-3-羧胺盐酸盐
英文名称	AT7519 Hydrochloride
英文别名	AT 7519;N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide hydrochloride;AT 7519 Hydrochloride;4-(2,6-Dichlorobenzoylamino)-1H-pyrazole-3-carboxylic Acid Piperidin-4-ylamide Monohydrochloride;4-[(2,6-dichlorobenzoyl)amino]-N-piperidin-4-yl-1H-pyrazole-5-carboxamide,hydrochloride;AT-7519;AT7519 (Hydrochloride);AT-7519 (hydrochloride);AT7519 HCl;AT-7519 HCl;AT-7519(HCl);AT7519.HCl;N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide Hcl;AT-7519 Hydrochloride;AT-7519M;QCR-194;AT7519 Hydrochloride;4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide hydrochloride;PubChem22417;AT7519(Hydrochloride);C16H17Cl2N5O2.HCl;AT7519(HCL);SYN1010;AOB2624;PAOFPNGYBWGKCO-UHFFFAOYSA-N;BCPP000382;BCP01950;s7808;1H-Pyrazole-3-carboxamide, 4-[(2,6-dichlorobenzoyl)amino]-N-4-piperidinyl-, monohydrochloride (9CI);4-(2,6-Dichlorobenzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide monohydrochloride;AT 7519 hydrochloride
Cas No.	902135-91-5
分子式	C₁₆H₁₈Cl₃N₅O₂
分子量	418.71
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

AT7519 Hydrochloride 是一种有效的 CDK 抑制剂，对 CDK1，CDK2，CDK4-CDK6 以及 CDK9 的 IC₅₀ 值分别为 210，47，100，13，170 和 <10 nM。

生物活性

AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC 50 s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.

性状

Solid

IC50 & Target[1][2]

CDK9/Cyclin T 10 nM (IC50) CDK5/p35 13 nM

体外研究(In Vitro)

AT7519 (0-4 μM) results in dose-dependent cytotoxicity with IC50s ranging from 0.5 to 2 μM in MM cells, and this induced cytotoxicity is associated with GSK-3β activation independent of transcriptional inhibition. AT7519 overcomes proliferative advantage conferred by cytokines and the protective effect of BMSC. AT7519 (0.5 μM) induces apoptosis of MM cells in a time-dependent manner. Moreover, AT7519 (0.5 μM) inhibits phosphorylation of RNA polymerase II CTD and partially inhibits RNA synthesis in MM.1S cells. AT7519 (250 nM) inhibits cell cycle progression in human tumor cell lines. AT7519 also induces apoptosis of human tumor cell lines. AT7519 (100-700 nM) induces apoptosis in leukemia cell lines. AT7519 also inhibits transcription in human tumor cell lines. Furthermore, AT7519 inhibits RNA polymerase II and reduces antiapoptotic protein levels.

体内研究(In Vivo)

AT7519 inhibits tumor growth in a human MM xenograft mouse model. AT7519 (4.6 and 9.1 mg/kg/dose) inhibits the growth of early-stage HCT116 tumor xenografts. AT7519 (10 mg/kg, i.p.) also inhibits the target CDKs in HCT116 tumor-bearing BALB/c nude mice. 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

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Santo L, et al. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition. Oncogene. 2010 Apr 22;29(16):2325-36.
[2]. Squires MS, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines.

溶解度数据	In Vitro: DMSO : ≥ 300 mg/mL (716.49 mM)H₂O : 8.33 mg/mL (19.89 mM; 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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