PKI-166 hydrochloride

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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 hydrochloride 

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

PKI-166 hydrochloride

PKI-166 hydrochloride Chemical Structure

CAS No. : 2230253-82-2

规格 是否有货
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PKI-166 hydrochloride 的其他形式现货产品:

PKI-166

生物活性

PKI-166 hydrochloride is a potent, selective and orally active 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)

PKI-166 hydrochloride (0-0.5 μM; 1 hour; pretreatment) inhibits EGFR autophosphorylation in human pancreatic cancer cells[1].
PKI-166 hydrochloride (0.03 μM; 6 days) enhances the cytotoxicity mediated by gemcitabine[1].

Shanghai Jinpan Biotech Co Ltd 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 hydrochloride (100 mg/kg; p.o.; daily; for 29 days) inhibits of pancreatic cancer growth[1].

Shanghai Jinpan Biotech Co Ltd 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; for 29 days
Result: Significantly decreased median tumor volume.

分子量

366.84

Formula

C20H19ClN4O
CAS 号

2230253-82-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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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