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JNJ28871063 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JNJ28871063 hydrochloride图片
CAS NO:944342-90-9
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitivepan-ErbB kinaseinhibitor withIC50values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in bothEGFRand ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpressEGFRand 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 IC50values 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].

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].

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.