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Submit ReviewPKI 166 hydrochloride is a potent EGFR-kinase inhibitor (IC50 = 0.7 nM). Displays >3000-fold selectivity against a panel of serine/threonine kinases. Reduces metastasis and angiogenesis in a mouse model of pancreatic cancer. Antihypertensive and orally bioavailable.
分子量 | 366.84 |
公式 | C20H18N4O.HCl |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2230253-82-2 |
PubChem ID | 91691117 |
InChI Key | ZPTWAAIZEGWMGX-BTQNPOSSSA-N |
Smiles | OC(C=C3)=CC=C3C2=CC1=C(N[C@@H]([C@]4=CC=CC=C4)C)N=CN=C1N2.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Bruns et al (2000) 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. 60 2926 PMID: 10850439
Ulu et al (2013) Epidermal growth factor receptor inhibitor PKI-166 governs cardiovascular protection without beneficial effects on the kidney in hypertensive 5/6 nephrectomized rats. J.Pharmacol.Exp.Ther. 345 393 PMID: 23528611
Kaspersen et al (2012) Activity of 6-aryl-pyrrolo[2,3-d]pyrimidine-4-amines to Tetrahymena. Bioorg.Chem. 44 35 PMID: 22832269
关键词: PKI 166 hydrochloride, PKI 166 hydrochloride supplier, 187724-61-4, potent, EGFR, kinase, inhibitors, epidermal, growth, factor, receptor, tyrosine, antiangiogenic, antitumor, antitumour, inhibits, PKI166, 4941, Tocris Bioscience
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