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BIBW2992(Tovok);
CAS:439081-18-2;
purity:98%
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Biological Activity of BIBW2992(Tovok):
In cell-free in vitro kinase assays, BIBW2992 shows potent activity against wild-type and mutant forms of EGFR and HER2, similar to gefitinib in potency for L858R EGFR, but about 100-fold more active against the gefitinib resistant L858R-T790M EGFR double mutant, with an IC50 of 10 nM. BIBW2992 was effective in inhibiting survival of lung cancer cell lines harboring wild-type (H1666) or L858R/T790M (NCI-H1975) EGFR, with IC50s below 100 nM for these isoforms resistant to first-generation inhibitors anda subnanomolar IC50 for the gefitinibsensitive L858R expressedby H3255.
Assessed in a standard xenograft model of the epidermoid carcinoma cell line A431.Daily oral treatment with BIBW2992 at 20 mg/kg for 25 days resulted in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%. [1]


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References on BIBW2992(Tovok):
[1] D Li et al. Oncogene.2008,27:4702–4711

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