PKI-166

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PKI-166  纯度: 98.78%

PKI-166 是一种高效、选择性的，有口服生物活性的 EGFR 酪氨酸激酶抑制剂，IC50 值为 0.7 nM。

PKI-166

PKI-166 Chemical Structure

CAS No. : 187724-61-4

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5 mg ￥5600 In-stock
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PKI-166 相关产品

•相关化合物库:

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生物活性

PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].

IC50 & Target

IC50: 0.7 nM (EGFR tyrosine kinase)[1]
体外研究
(In Vitro)

Pretreatment with PKI-166 (0-0.5 μM; 1 hour) inhibits EGFR autophosphorylation in human pancreatic cancer cells[1].
PKI-166 (0.03μ M; 6 days) enhanced the cytotoxicity mediated by gemcitabine[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: L3.6pl cells
Concentration: 0.01 μM, 0.05 μM, 0.5 μM
Incubation Time: 1 hour
Result: Inhibited EGFR autophosphorylation in a dose-dependent manner.

Cell Cytotoxicity Assay[1]

Cell Line: L3.6pl cells
Concentration: 0.03 μM
Incubation Time: 6 days
Result: Enhanced the cytotoxicity mediated by gemcitabine.

体内研究
(In Vivo)

PKI-166 (100 mg/kg; p.o.; daily; day 7-day 35 after xenograft) inhibits of pancreatic cancer growth[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic nude mice with L3.6pl cells xenograft (8–12 weeks)[1]
Dosage: 100 mg/kg
Administration: Oral administration; daily; from day 7 to day 35 after xenograft
Result: Significantly decreased median tumor volume.

分子量

330.38

Formula

C20H18N4O
CAS 号

187724-61-4
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
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Bruns CJ, et al. Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 2000 Jun 1;60(11):2926-35.

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