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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.
M. Wt | 516.87 |
Formula | C22H27ClFN7.2HCl |
Storage | Desiccate at +4°C |
Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
Solca et al (2004) Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. J.Pharmacol.Exp.Ther. 311 502 PMID: 15199094
Keywords: BIBU 1361 dihydrochloride, BIBU 1361 dihydrochloride supplier, Selective, inhibitors, inhibits, EGFR-kinases, Epidermal, Growth, Factors, Receptors, ErbB, Her, Receptor, Tyrosine, Kinases, RTKs, BIBU1361, dihydrochloride, EGFR, 2417, Tocris Bioscience
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