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BIBW2992

Cat. No. M1677
BIBW2992 Structure
Synonym:

Afatinib,Tomtovok, Tovok

Size Price Availability Quantity
10mg USD 60 In stock
50mg USD 130 In stock
100mg USD 200 In stock
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Quality Control
Biological Activity

BIBW2992 (Afatinib) is a novel irreversible dual EGFR and HER2 tyrosine kinase inhibitor. The potency of BIBW2992 on the EGFR and HER2 kinases revealed IC50 values of 0.5 nM and 14 nM, respectively. BIBW2992 suppresses transformation in isogenic cell-based assays, inhibits survival of cancer cell lines and induces tumor regression in xenograft and transgenic lung cancer models, with superior activity over erlotinib.

Protocol
Cell Experiment
Cell lines NSCLC cells H1666, H3255 and NCI-H1975
Preparation method Growth inhibition of lung cancer cell lines by BIBW2992 and other EGFR and/or HER2 inhibitors (a) Sensitivity of NSCLC cell lines that express EGFR WT, Exon 19 Del, L858R/ T790M and HER2 INS776V to BIBW2992 and erlotinib. Dose-dependent growth inhibition was determined by MTS assay. Only HCC827 cells are sensitive to erlotinib whereas NCIH1781 and NCI-H1975 cells are also sensitive to BIBW2992. Points, average of two independent experiments, each done in triplicate; bars, s.d. *A549 cells harbor a Kras G12S mutation. See also in Supplementary Table 4. (b) Inhibition of anchorage independent cell proliferation of various lung cancer cell lines treated with BIBW2992, lapatinib, canertinib, gefitinib or erlotinib. The IC50 values were determined as described.
Concentrations 0~10µM
Incubation time 72 h
Animal Experiment
Animal models A431 cells mouse bearing tumor xenograft model
Formulation 0.5% methocellulose-0.4% polysorbate-80 (Tween 80)
Dosages 20 ml/kg body weight once daily
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 485.94
Formula C24H25ClFN5O3
CAS Number 439081-18-2
Purity >99%
Solubility DMSO
Storage at -20°C
References

A phase II trial to assess efficacy and safety of afatinib in extensively pretreated patients with HER2-negative metastatic breast cancer.
Schuler et al. Breast Cancer Res Treat. 2012 Aug;134(3):1149-59. PMID: 22763464.

A phase II study of afatinib (BIBW 2992), an irreversible ErbB family blocker, in patients with HER2-positive metastatic breast cancer progressing after trastuzumab.
Lin et al. Breast Cancer Res Treat. 2012 Jun;133(3):1057-65. PMID: 22418700.

Clinical activity of afatinib (BIBW 2992) in patients with lung adenocarcinoma with mutations in the kinase domain of HER2/neu.
De Grève et al. Lung Cancer. 2012 Apr;76(1):123-7. PMID: 22325357.

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  Catalog
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Keywords: BIBW2992, Afatinib,Tomtovok, Tovok supplier, EGFR/HER2, inhibitors

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