Afatinib (BIBW 2992)

Cat. No. M1677

Synonym:

BIBW2992, Tomtovok, Tovok, CAS# 439081-18-2

Size	Price	Availability
Free Sample (0.5-1 mg)	USD 0	In stock
10mM*1mL	USD 63 USD63	In stock
5mg	USD 43 USD43	In stock
10mg	USD 71 USD71	In stock
50mg	USD 105 USD105	In stock

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Quality Control & Documentation

Purity: 98.42%
COA
MSDS
H-NMR
HPLC

Product Information

Biological Activity

Afatinib (BIBW 2992) is a novel irreversible dual EGFR and HER2 tyrosine kinase inhibitor. The potency of Afatinib (BIBW 2992) on the EGFR and HER2 kinases revealed IC50 values of 0.5 nM and 14 nM, respectively. Afatinib (BIBW 2992) 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# 439081-18-2

Product Citations

Clin Transl Oncol. 2023 May;25(5):1425-1435.

ADAM12 promotes gemcitabine resistance by activating EGFR signaling pathway and induces EMT in bladder cancer
Afatinib (BIBW 2992) purchased from AbMole
J Virol. 2020 Feb 14;94(5):e01791-19.

Targeting Kaposi's Sarcoma-Associated Herpesvirus ORF21 Tyrosine Kinase and Viral Lytic Reactivation by Tyrosine Kinase Inhibitors Approved for Clinical Use
Afatinib (BIBW 2992) purchased from AbMole

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 (for reference only)

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

Chemical Information

Molecular Weight	485.94
Formula	C24H25ClFN5O3
CAS Number	850140-72-6
Form	Solid
Solubility (25°C)	DMSO ≥ 80 mg/mL
Storage	Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month

Conversion of different model animals based on BSA (PMID: 27057123)

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
K_m factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B K_m
	Animal A K_m

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 K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Schuler et al. Breast Cancer Res Treat. A phase II trial to assess efficacy and safety of afatinib in extensively pretreated patients with HER2-negative metastatic breast cancer.

[2] Lin et al. Breast Cancer Res Treat. A phase II study of afatinib (BIBW 2992), an irreversible ErbB family blocker, in patients with HER2-positive metastatic breast cancer progressing after trastuzumab.

[3] De Grève et al. Lung Cancer. Clinical activity of afatinib (BIBW 2992) in patients with lung adenocarcinoma with mutations in the kinase domain of HER2/neu.

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