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Submit ReviewBIBU 1361 dihydrochloride is a potent inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 3 nM). Displays ~ 100-fold lower potency against ErbB2 (IC50 = 290 nM) and is selective over a range of other related tyrosine kinases (IC50 > 10 μM). Blocks downstream EGFR signaling events such as MAPKK/MAPK activation. Oral administration inhibits growth of established human xenografts in athymic mice.
分子量 | 516.87 |
公式 | C22H27ClFN7.2HCl |
储存 | Desiccate at +4°C |
纯度 | ≥97% (HPLC) |
CAS Number | 1643609-75-9 |
PubChem ID | 46861539 |
InChI Key | ZNNWCQCQUKAMGL-UHFFFAOYSA-N |
Smiles | Cl.Cl.CCN(CC)CC1CCN(CC1)C1=NC=C2N=CN=C(NC3=CC(Cl)=C(F)C=C3)C2=N1 |
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。
Solca et al (2004) Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. J.Pharmacol.Exp.Ther. 311 502 PMID: 15199094
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