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BIBW2992

Cat. No. M1677
BIBW2992 Structure
Synonym:

Afatinib, Tomtovok, Tovok, CAS# 850140-72-6

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL USD 56.7  USD63 In stock
5mg USD 38.7  USD43 In stock
10mg USD 63.9  USD71 In stock
50mg USD 94.5  USD105 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Another CAS# 850140-72-6

Product Citations
Customer Product Validations & Biological Datas
Source Am J Cancer Res (2015). Figure 3. BIBW2992
Method Western Blot
Cell Lines HKESC-2 and EC-1 cell lines
Concentrations 0.1 μM
Incubation Time 24 h
Results In HKESC-2 and EC-1 cell lines, afatinib could suppress AKT phosphorylation in a dose and time dependent manner, in which the phosphorylation was almost completely abrogated when the cells were treated with concentrations around their corresponding IC50 (HKESC-2: 0.1 μM, EC-1: 1 μM) for 24 hours (Figure 3).
Source Am J Cancer Res (2015). Figure 1. BIBW2992
Method ELISA
Cell Lines ESCC cell lines
Concentrations 0.1 μM
Incubation Time 48 and 72 h
Results All 5 ESCC cell lines were sensitive to afatinib, in which over 95% of growth inhibition was observed after 48 and 72 hours of treatment (Figure 1B).
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 485.94
Formula C24H25ClFN5O3
CAS Number 439081-18-2
Purity >99%
Solubility DMSO ≥ 80 mg/mL
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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Keywords: BIBW2992, Afatinib, Tomtovok, Tovok, CAS# 850140-72-6 supplier, EGFR/HER2, inhibitors

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