Product Information Novel Life Science Reagents

for Cell Signaling Research

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Technical Data:
Orders
M.Wt: 485.94 F +1-713-922-4115
Formula: C24H25ClFN5O3 Cl NH enquiry@selleckchem.com
H
Solubility: DMSO N
N
N

Purity: 99% N O
O Tech Support
tech@selleckchem.com
Storage: at -20℃ 2 years O (chemistry support)
CAS No.: 439081-18-2 Synonyms: Tovok techbio@selleckchem.com
(bio support)

Web
Biological Activity
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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
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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 Please inspect packages immediately upon

receipt and notify customer service within

[1] D Li et al. Oncogene.2008,27:4702–4711 3 days of delivery of any damage or

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