PKI 166 hydrochloride

Cat. No. 4941 提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent EGFR-kinase inhibitor

化学名： 4-[4-[[(1R)-1-Phenylethyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenol hydrochloride

纯度： ≥98% (HPLC)

文献 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for PKI 166 hydrochloride

PKI 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.

技术数据 for PKI 166 hydrochloride

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.

溶解性数据 for PKI 166 hydrochloride

	溶剂	最高浓度 mM
溶解性
	DMSO	100
	ethanol	50

制备储备液 for PKI 166 hydrochloride

以下数据基于产品分子量 366.84。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	2.73 mL	13.63 mL	27.26 mL
5 mM	0.55 mL	2.73 mL	5.45 mL
10 mM	0.27 mL	1.36 mL	2.73 mL
50 mM	0.05 mL	0.27 mL	0.55 mL

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产品说明书 for PKI 166 hydrochloride

分析证书/产品说明书

化学品安全技术说明书

参考文献 for PKI 166 hydrochloride

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

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