JNJ28871063 hydrochloride

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。

JNJ28871063 hydrochloride 

JNJ28871063 hydrochloride 是一种口服有效、高选择性和 ATP 竞争性的 pan-ErbB 激酶抑制剂,对 ErbB1、ErbB2 和 ErbB4 的 IC50 值分别为 22 nM、38 nM 和 21 nM。JNJ28871063 hydrochloride 抑制 EGFR 和 ErbB2 中具有重要功能的酪氨酸残基的磷酸化。JNJ28871063 hydrochloride 可以透过血脑屏障,在过表达 EGFR 和 ErbB2 的人类肿瘤异种移植模型中具有抗肿瘤活性。

JNJ28871063 hydrochloride

JNJ28871063 hydrochloride Chemical Structure

CAS No. : 944342-90-9

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生物活性

JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2[1].

IC50 & Target[1]

ErbB1

22 nM (IC50)

ErbB2

38 nM (IC50)

ErbB4

21 nM (IC50)

体外研究
(In Vitro)

JNJ-28871063 demonstrates potent growth inhibition in vitro of human cancer cell lines (N87; BT474; SKBR3; A431; HN5) overexpressing the ErbB2 receptor with IC50 values with 60-168 nM. 28871063 exhibited the least effect at inhibiting growth of non–ErbB-over-expressing cell lines (HeLa, A375, HCT116, HT29, MRC5 primary fibroblasts cells; IC50>10 μM)[1].
JNJ-28871063 hydrochloride (3 μM; 16 hours) reduces the basal level of ErbB2 phosphorylation in SKBR3 cells[1].
JNJ28871063 hydrochloride is from an aminopyrimidine oxime structural class[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: BT474 cells
Concentration: 3 μM
Incubation Time: 16 hours
Result: Reduced the basal level of ErbB2 phosphorylation.

体内研究
(In Vivo)

JNJ28871063 hydrochloride (100 mg/kg/day; Oral; for 30 days) shows significant inhibition of tumor growth (TGI=71%)[1].
JNJ28871063 hydrochloride produces a significant inhibition of tumor growth at 100 mg/kg (TGI=66.8%) in an A431 human tumor xenograft model[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice bearing N87 tumor xenografts[1]
Dosage: 100 mg/kg
Administration: Oral; daily for 30 days
Result: Showed significant inhibition of tumor growth (TGI=71%).

分子量

519.42

Formula

C24H28Cl2N6O3

CAS 号

944342-90-9

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]. Stuart L Emanuel, et al. Cellular and in vivo activity of JNJ-28871063, a nonquinazoline pan-ErbB kinase inhibitor that crosses the blood-brain barrier and displays efficacy against intracranial tumors. Mol Pharmacol. 2008 Feb;73(2):338-48.

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