Afatinib oxalate (Synonyms: BIBW 2992 oxalate)

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Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC₅₀ values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR^wt, EGFR^L858R, EGFR^L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.

For research use only. We do not sell to patients.

Afatinib oxalate Chemical Structure

CAS No. : 1398312-64-5

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Other In-stock Forms of Afatinib oxalate:

Afatinib Afatinib dimaleate

Other Forms of Afatinib oxalate:

Afatinib In-stock
Afatinib dimaleate In-stock
(E/Z)-Afatinib Get quote
Afatinib-d₆ Get quote

60 Publications Citing Use of MCE Afatinib oxalate

: Afatinib oxalate purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Apr;109(4):1166-1176. [Abstract]; Influence of Afatinib or Neratinib on human epidermal growth factor receptor 2 (HER2) and the downsignal pathway in gastric cancer cell lines.

: Afatinib oxalate purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Mar;17(3):603-613. [Abstract]; Immunoblot analysis of U-CH1, MUG-Chor1 and Chor-IN-1 cells treated with Afatinib for 2 h or 48 h. Protein cell extracts are resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC₅₀s for each cell line are reported.

: Afatinib oxalate purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Mar;17(3):603-613. [Abstract]; Immunoblot analysis of U-CH1 cells treated with the indicated doses of inhibitors (Afatinib, Erlotinib and Lapatinib) for 2 h (upper panel) or 48 h (lower panel). Protein cell extracts are resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC₅₀s of the different inhibitors are reported.

: Afatinib oxalate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2014 Dec 15;5(23):11971-85. [Abstract]; H460/MX20 cells are treated with varying concentrations (0–2.0 μM) of Afatinib for 48 h, or with 1.0 μM Afatinib for 24 h, 48 h and 72 h, respectively. ABCG2 protein levels are analyzed by Western blot. GAPDH is used as a loading control.

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

EGFR^L858R

0.4 nM (IC₅₀)

EGFR^WT

0.5 nM (IC₅₀)

EGFR^L858R/T790M

10 nM (IC₅₀)

HER2

14 nM (IC₅₀)

HER3

In Vitro

Afatinib oxalate (100 nM) sufficiently prevents heregulin-stimulated HER3 phosphorylation^[1].
Afatinib oxalate (0-10000 nM) effectively inhibits anchorage-independent proliferation of NIH-3T3 cells ectopically expressing EGFR mutants, and inhibits cell proliferation of H1666, H3255, and NCI 1975 cells^[1].
Afatinib oxalate (48-72 h)shows growth inhibition in HKESC-1, HKESC-2, SLMT-1 and EC-1 cells^[2].
Afatinib oxalate (0-1 μM, 24-48 h) inhibits AKT and MAPK pathways, and inhibits EGFR and AKT phosphorylation in ESCC cell lines^[2].
Afatinib oxalate (0-1 μM, 16-48 h) induces G0/G1 cell cycle arrest in HKESC-2 and EC-1^[2].
Afatinib oxalate (0-1 μM, 24-48 h) effectively induces apoptotic cell death in HKESC-2 and EC-1^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	NIH-3T3 cells, H1666, H3255, and NCI 1975 cells
Concentration:	0, 1, 10, 100, 1000, 10000 nM
Incubation Time:
Result:	Effectively inhibited anchorage-independent proliferation of NIH-3T3 cells ectopically expressing EGFR mutants. Showed inhibition of anchorage independent cell proliferation of various lung cancer cell lines (H1666, H3255, and NCI 1975 cells), with IC₅₀ values of 60 nM, 0.7 nM and 99 nM, respectively.

Cell Viability Assay^[2]

Cell Line:	HKESC-1, HKESC-2, SLMT-1 and EC-1 cell lines
Concentration:
Incubation Time:	48 and 72 hours
Result:	Observed over 95% of growth inhibition. The respective IC₅₀ concentrations at 48 hours (HKESC-1=0.078 μM, HKESC-2=0.115 μM, KYSE510=3.182 μM, SLMT-1=4.625 μM and EC-1=1.489 μM) and 72 hours (HKESC-1=0.002 μM, HKESC-2=0.002 μM, KYSE510=1.090 μM, SLMT-1=1.161 μM and EC-1=0.109 μM) were all in lower micro-molar range.

Western Blot Analysis^[2]

Cell Line:	HKESC-2 cells and EC-1 cells
Concentration:	0, 0.01, and 0.1 μM (HKESC-2 cells), 0, 0.1 and 1 μM (EC-1 cells)
Incubation Time:	24 and 48 hours
Result:	Reduced the phosphorylation of EGFR and the endogenous expression level of HER2 receptors in ESCC cells. Suppressed AKT phosphorylation in a dose and time dependent manner. Significantly reduced the phosphorylation level of the downstream effectors of the AKT-mTOR axis especially in HKESC-2 cells. Inhibited the two major downstream pathways of the ErbB/HER axis, namely, AKT and MAPK pathways in ESCC cell lines.

Cell Cycle Analysis^[2]

Cell Line:	HKESC-2 cells and EC-1 cells
Concentration:	0, 0.01, and 0.1 μM (HKESC-2 cells), 0, 0.1 and 1 μM (EC-1 cells)
Incubation Time:	16, 24, and 48 hours
Result:	Induced G0/G1 cell cycle arrest in both tested ESCC cell lines in a time and dose dependent manner. In HKESC-2 cells, the percentage of cells in G0/G1 phase was increased from 38.2% to 68.1% at 0.01 μM of afatinib and to 74.7% at 0.1 μM of afatinib, from 24 hours (82.4% G0/G1 arrest at 0.01 μM and 86.2% at 0.1 μM) to 48 hours (from 74.7% to 88.2% for 0.01 μM and 91.0% for 0.1 μM). In EC-1 cells, the percentage of cells arrested in the G0/G1 phase was increased from 59.1% to 66.6% and 72.2% at 24 and 48 hours respectively.

Apoptosis Analysis^[2]

Cell Line:	HKESC-2 cells and EC-1 cells
Concentration:	0, 0.01, and 0.1 μM (HKESC-2 cells), 0, 0.1 and 1 μM (EC-1 cells)
Incubation Time:	24 and 48 hours
Result:	Effectively induced cell death by triggering apoptotic mechanisms in ESCC cell lines. Showed a stronger expression level of cleaved Poly (ADP-ribose) polymerase (PARP) in these cell lines.

In Vivo

Afatinib oxalate (0-20 mg/kg, Orally, daily for 25 days) shows dramatic tumor regression and downregulation of EGFR, HER2, HER3 and AKT phosphorylation^[1].
Afatinib oxalate (15 mg/kg, Orally, in a schedule of 5 days on plus 2 days off, for two weeks) strongly inhibits the growth of HKESC-2 tumor^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Athymic NMRI-nu/nu female mice (21–31 g, five to six-week-old, transgenic murine lung cancer model and xenograft models)^[1]
Dosage:	15 mg/kg, 20 mg/kg
Administration:	Orally, daily for 25 days
Result:	Resulted in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2% in a standard xenograft model of the epidermoid carcinoma cell line A431, and downregulation of EGFR and AKT phosphorylation. Induced regression of large tumors in this HER2-driven model, effectively controlled xenograft tumor formation by the NCIH1975 cell line, expressing EGFR L858R/T790M, with a T/C value of 12% for doses of 20 mg/kg. Induced more than 50% percent tumor reduction after a 4-week treatment period. Downregulated EGFR, HER2 and HER3 phosphorylation.

Animal Model:	Six weeks old female athymic nude mice (nu/nu) (16-20 g)^[2]
Dosage:	15 mg/kg
Administration:	Oral gavage in a schedule of 5 days on plus 2 days off, for two weeks
Result:	Strongly inhibited the growth of HKESC-2 tumor. Average tumor sizes of vehicle and treatment at end point are 348 ± 24 mm³ and 108 ± 36 mm³ respectively.

Clinical Trial

Molecular Weight

575.97

Formula

C₂₆H₂₇ClFN₅O₇

CAS No.

1398312-64-5

SMILES

OC(C(O)=O)=O.CN(C)C/C=C/C(NC1=CC(C(NC2=CC(Cl)=C(C=C2)F)=NC=N3)=C3C=C1O[C@H]4CCOC4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Li D, et al. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008 Aug 7;27(34):4702-11. [Content Brief]

[2]. Wong CH, et al. Preclinical evaluation of afatinib (BIBW2992) in esophageal squamous cell carcinoma (ESCC). Am J Cancer Res. 2015 Nov 15;5(12):3588-99. [Content Brief]

[3]. Wang XK, et al. Afatinib circumvents multidrug resistance via dually inhibiting ATP binding cassette subfamily G member 2 in vitro and in vivo. Oncotarget. 2014 Dec 15;5(23):11971-85. [Content Brief]

[4]. Yoshioka T, et al. Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. Cancer Sci. 2018 Apr;109(4):1166-1176. [Content Brief]

Afatinib oxalate Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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