Pelitinib|257933-82-7|(培利替尼; EKB-569; WAY-EKB 569)-陌孚医药/Medlife

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Pelitinib (Synonyms: 培利替尼; EKB-569; WAY-EKB 569)

目录号: PL05021 纯度: ≥98%

CAS No. :257933-82-7

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中文名称	Pelitinib
中文别名	培利替尼;贝利替尼;(2E)-N-[4-[(3-氯-4-氟苯基)氨基]-3-氰基-7-乙氧基-6-喹啉基]-4-(二甲基氨基)-2-丁烯酰胺;Pelitinib (EKB-569) 抑制剂;培利替尼（Pelitinib）;培利替尼贝利替尼Pelitinib EKB-569;萘哌地尔双盐酸;培利替尼 (2E)-N-[4-[(3-氯-4-氟苯基)氨基]-3-氰基-7-乙氧基-6-喹啉基]-4-二甲氨基-2-丁烯酰胺
英文名称	Pelitinib
英文别名	Pelitinib;(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide;(E)-N-(4-(3-Chloro-4-fluorophenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide;Dacomitinib;EKB569;EKB-569;Pelitinib (EKB-569); (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethy;(2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-buteneamide;4-dimethylamino-but-2-enoic acid [4-(3-chloro-4-fluoro-phenylamino)-3-cyano-7-ethoxy-quinolin-6-yl]-amide;WAY-EKB 569;WAY-EKB-569;(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-dimethylamino-2-butenamide;EKB 569;C24H23ClFN5O2;X5DWL380Z6;(2E)-N-{4-[(3-chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxyquinolin-6-yl}-4-(dimethylamino)but-2-enamide;(2E)-N-(4-((3-chloro-4-fluorophenyl)amino)-3-cyano-7-ethoxy-6-quinolinyl)-4-(dimethylamino)-2-butenamide;(E)-N-[4-[(3-chloranyl-4-
Cas No.	257933-82-7
分子式	C₂₄H₂₃ClFN₅O₂
分子量	467.92
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Pelitinib (EKB-569;WAY-EKB 569) 是可逆的 EGFR 抑制剂，IC₅₀ 值为38.5 nM。也可轻微抑制Src，MEK/ERK 和 ErbB2，IC₅₀ 值分别为282，800，和1255 nM。

生物活性

Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC 50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC 50 s of 282, 800, and 1255 nM, respectively.

性状

Solid

IC50 & Target[1][2]

EGFR 38.5 nM (IC50)

体外研究(In Vitro)

Pelitini has much greater inhibitory activity against the EGFR kinase than against Src, MEK/ERK, Cdk4, c-Met, Raf and ErbB2, for example, the IC50 for EGFR is 32-fold lower than the IC50 for the closely related ErbB2. Pelitinib results in a dramatic reduction in EGFR phosphorylation but no change in the total amount of EGFR protein. It requires at least 10-fold more drug to equivalently inhibit ErbB2 phosphorylation in similar assays, and EKB-569 does not block phosphorylation of another receptor tyrosine kinase (c-Met) assessed in the same manner. EKB-569 is a potent inhibitor of proliferation in NHEK, A431, and MDA-468 cells (IC50=61, 125, and 260 nM, respectively) but not MCF-7 cells (IC50=3600 nM). EKB-569 is also a potent inhibitor of EGF-induced phosphorylated EGF-R (pEGF-R) in A431 and NHEK cells (IC50=20-80 nM).

体内研究(In Vivo)

A single oral dose of 10 mg/kg EKB-569 inhibits EGFR phosphorylation in A431 xenografts within 60 minutes. Twenty-four hours later, EGFR activity is still inhibited by over 50% by this single oral dose. The half-life of EKB-569 in mouse plasma is about 2 hours. 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

ClinicalTrial

参考文献

[1]. Torrance CJ, et al. Combinatorial chemoprevention of intestinal neoplasia. Nat Med. 2000 Sep;6(9):1024-8.
[2]. Nunes M, et al. Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes. Mol Cancer Ther. 2004 Jan;3(1):21-7.

溶解度数据	In Vitro: DMSO : 25 mg/mL (53.43 mM; Need ultrasonic)配制储备液

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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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