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Submit ReviewJNJ 28871063 hydrochloride is a potent and selective ErbB receptor family inhibitor (IC50 values are 21, 22 and 38 nM for ErbB4, EGFR and ErbB2 respectively). Displays potent growth inhibition of human cancer cell lines overexpressing ErbB2 in vitro (IC50 = 60 - 168 nM) and inhibits growth of human tumor xenografts in vivo. Brain penetrant and orally active.
JNJ 28871063 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 519.42 |
公式 | C24H27ClN6O3.HCl |
储存 | Desiccate at +4°C |
纯度 | ≥97% (HPLC) |
CAS Number | 944342-90-9 |
PubChem ID | 17747413 |
InChI Key | ZXKZRKQMKNRZNN-GZPZNDDGSA-N |
Smiles | NC1=C(/C=N/OCCN2CCOCC2)C(NC3=CC(Cl)=C(OCC4=CC=CC=C4)C=C3)=NC=N1.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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 25.97 | 50 |
以下数据基于产品分子量 519.42。 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 |
---|---|---|---|
0.5 mM | 3.85 mL | 19.25 mL | 38.5 mL |
2.5 mM | 0.77 mL | 3.85 mL | 7.7 mL |
5 mM | 0.39 mL | 1.93 mL | 3.85 mL |
25 mM | 0.08 mL | 0.39 mL | 0.77 mL |
参考文献是支持产品生物活性的出版物。
Contessa and Hamstra (2008) Revoking the privilege: targeting HER2 in the central nervous system. Mol.Pharmacol. 73 271 PMID: 17981994
Emanuel et al (2008) 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. 73 338 PMID: 17975007
Guessous et al (2008) Signaling pathways in medulloblastoma. J.Cell.Phys. 217 577 PMID: 18651559
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