Cat. No.: HY-10261A

Afatinib dimaleate

(Synonyms: BIBW 2992MA2)

107 Cited Publications

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Based on 107 publication(s) in Google Scholar

Afatinib (BIBW 2992) dimaleate 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 dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 99.74%
CAS No.: 850140-73-7
Formule: C₃₂H₃₃ClFN₅O₁₁
Masse moléculaire:718.08

Stockage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Afatinib dimaleate Chemical Structure

CAS No.: 850140-73-7

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (107)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
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Activité biologique

Description

IC₅₀ & Target^[1]

EGFR^L858R

0.4 nM (IC₅₀)

EGFR

0.5 nM (IC₅₀)

EGFR^L858R/T790M

10 nM (IC₅₀)

HER2

14 nM (IC₅₀)

HER3

Voir tous les produits spécifiques à Isoform EGFR :

Voir tous les produits spécifiques à Isoform Akt :

Voir tous les produits spécifiques à Isoform p38 MAPK :

In Vitro

Afatinib dimaleate (100 nM) sufficiently prevents heregulin-stimulated HER3 phosphorylation^[1].
Afatinib dimaleate (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 dimaleate (48-72 h)shows growth inhibition in HKESC-1, HKESC-2, SLMT-1 and EC-1 cells^[2].
Afatinib dimaleate (0-1 μM, 24-48 h) inhibits AKT and MAPK pathways, and inhibits EGFR and AKT phosphorylation in ESCC cell lines^[2].
Afatinib dimaleate (0-1 μM, 16-48 h) induces G0/G1 cell cycle arrest in HKESC-2 and EC-1^[2].
Afatinib dimaleate (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 dimaleate (0-20 mg/kg, Orally, daily for 25 days) shows dramatic tumor regression and downregulation of EGFR, HER2, HER3 and AKT phosphorylation^[1].
Afatinib dimaleate (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.

Chemical Information

CAS No. 850140-73-7
Appearance Solid
Masse moléculaire 718.08
Formule C₃₂H₃₃ClFN₅O₁₁
Color White to yellow
SMILES

O=C(NC1=C(C=C2C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)=C1)O[C@H]4CCOC4)/C=C/CN(C)C.O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O
Synonyms

BIBW 2992MA2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (107)

All WBFlow CytometryIn Vivo Efficacy StudyIHCOthersCell Proliferation/Viability AssayRT-PCR

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Nature

Inhibitors supercharge kinase turnover through native proteolytic circuits. [Abstract]

2026 Jan;649(8098):1032-1041. PMID: 41299171

Afatinib dimaleate purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1032-1041. [Abstract]

Immunoblot analysis of cell lines (K562 HER2WT or HER2C805S Nluc-3xFLAG reporter cell lines) treated for 15 h with AV-412 (HY-10346; 2.5 µM), neratinib (HY-32721; 10 µM), afatinib (HY-10261; 10 µM), WZ4002 (HY-12026; 10 µM).

Afatinib dimaleate purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1032-1041. [Abstract]

Luminescent reporter assay of K562 HER2WT or HER2C805S Nluc-3xFLAG reporter cell lines treated for 15 h with the indicated compounds (AV-412 (HY-10346; 2.5 µM), neratinib (HY-32721; 10 µM), afatinib (HY-10261; 10 µM), WZ4002 (HY-12026; 10 µM)) shown as normalized luminescence per genetic construct (two-way ANOVA, Sidak corrected) (n = 3).
Cancer Cell

2026 May 21:S1535-6108(26)00220-5. PMID: 42167227
Cancer Cell

Anti-tumor efficacy of HRS-4642 and its potential combination with proteasome inhibition in KRAS G12D-mutant cancer. [Abstract]

2024 Jul 8;42(7):1286-1300.e8. PMID: 38942026
Cancer Cell

KMT2D deficiency drives lung squamous cell carcinoma and hypersensitivity to RTK-RAS inhibition. [Abstract]

2023 Jan 9;41(1):88-105.e8. PMID: 36525973

Afatinib dimaleate purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2023 Jan 9;41(1):88-105.e8. [Abstract]

Cell viability assays of Kmt2d KO LUSC cell lines, Kmt2d WT LUSC cell lines, and LUAD (KP) cell line treated with afatinib for 72h. Data presented as mean ± SD (n = 3). The calculated IC50 values of afatinib is shown below.
J Hematol Oncol

SMARCA4 controls state plasticity in small cell lung cancer through regulation of neuroendocrine transcription factors and REST splicing. [Abstract]

2024 Jul 30;17(1):58. PMID: 39080761
Cancer Discov

Tumor-Intrinsic Kinome Landscape of Pancreatic Cancer Reveals New Therapeutic Approaches. [Abstract]

2025 Feb 7;15(2):346-362. PMID: 39632628
Nat Genet

Loss of Kmt2c or Kmt2d primes urothelium for tumorigenesis and redistributes KMT2A-menin to bivalent promoters. [Abstract]

2025 Jan;57(1):165-179. PMID: 39806204

Afatinib dimaleate purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Jan;57(1):165-179. [Abstract]

Afatinib (10 mg/kg/day; daily, 5 days per week by oral gavage) decreased the intensity of EGFR phosphorylation (pY845) in NOD-SCID mice.

Afatinib dimaleate purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Jan;57(1):165-179. [Abstract]

Afatinib (10 mg/kg/day; daily, 5 days per week by oral gavage) reduced the number of Ki-67-positive proliferating cells in NOD-SCID mice.
Nat Cell Biol

Growth factor-triggered de-sialylation controls glycolipid-lectin-driven endocytosis. [Abstract]

2025 Mar;27(3):449-463. PMID: 39984654
Cancer Res

C-terminal Truncation and Fusion Partner Determine Oncogenicity of FGFR3. [Abstract]

2025 Dec 29. PMID: 41460723
Cancer Res

NF1 Loss Promotes EGFR Activation and Confers Sensitivity to EGFR Inhibition in NF1 Mutant Melanoma. [Abstract]

2025 Jun 10:10.1158/0008-5472.CAN-24-3904. PMID: 40494652

Afatinib dimaleate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Jun 10:10.1158/0008-5472.CAN-24-3904. [Abstract]

Growth curves of NF1^Mut melanoma STCs treated with 0.1, 0.5, 1, 5, or 10 μM Afatinib.

Afatinib dimaleate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Jun 10:10.1158/0008-5472.CAN-24-3904. [Abstract]

Growth curves of NF1^Mut melanoma STCs treated with 0.1, 0.5, 1, 5, or 10 μM Afatinib.
Mol Cell

Amplified dosage of the NKX2-1 lineage transcription factor controls its oncogenic role in lung adenocarcinoma. [Abstract]

2025 Mar 21:S1097-2765(25)00194-7. PMID: 40139189
Cancer Res

Targeting c-Myc to Overcome Acquired Resistance of EGFR Mutant NSCLC Cells to the Third-Generation EGFR Tyrosine Kinase Inhibitor, Osimertinib. [Abstract]

2021 Sep 15;81(18):4822-4834. PMID: 34289988
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

An alternative EGFR activation by patient-derived R252C mutation promotes cancer progression. [Abstract]

2026 Jan 21;17(1):1902. PMID: 41565660
Nat Commun

Fructose intake driven glycolysis-ROS-EGFR axis specifically promotes the generation and pathogenicity of Th17 cells. [Abstract]

2025 Nov 23;16(1):11115. PMID: 41276507
Nat Commun

PPARα-mediated lipid metabolism reprogramming supports anti-EGFR therapy resistance in head and neck squamous cell carcinoma. [Abstract]

2025 Feb 1;16(1):1237. PMID: 39890801

Afatinib dimaleate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1237. [Abstract]

mRNA expression for CPT1A in cetuximab-sensitive (-S) and -resistant (-R) FaDu cells upon treatment with gefitinib, afatinib, selumetinib or buparlisib (2 µM each, for 24 h) (N = 3, n = 3).

Afatinib dimaleate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1237. [Abstract]

mRNA expression for CPT1A in cetuximab-sensitive (-S) and -resistant (-R) SC263 cells upon treatment with gefitinib, afatinib, selumetinib or buparlisib (2 µM each, for 24 h) (N = 3, n = 3).
Nat Commun

AURKB as a target in non-small cell lung cancer with acquired resistance to anti-EGFR therapy. [Abstract]

2019 Apr 18;10(1):1812 PMID: 31000705
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Chem Eng J

2024 May 15, 488, 150822.
Biomaterials

Automated discovery of nanomaterials via drug aggregation induced emission. [Abstract]

2022 Oct:289:121800. PMID: 36166893
J Exp Clin Cancer Res

Pyrotinib targeted EGFR/GRP78 mediated cell apoptosis in high EGFR gene copy number gastric cancer. [Abstract]

2025 Aug 19;44(1):245. PMID: 40830980
J Exp Clin Cancer Res

Dual inhibition of HERs and PD-1 counteract resistance in KRASG12C-mutant head and neck cancer. [Abstract]

2024 Nov 20;43(1):308. PMID: 39567998
J Exp Clin Cancer Res

The potential of swine pseudorabies virus attenuated vaccine for oncolytic therapy against malignant tumors. [Abstract]

2023 Oct 27;42(1):284. PMID: 37891570
Redox Biol

C-terminal interleukin 1 alpha (IL-1α) overexpression drives EMT and a vulnerability to ferroptosis in HNSCC. [Abstract]

2026 Jun:93:104172. PMID: 42013543
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 2:102053. PMID: 40187357
Cell Rep Med

Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]

2023 Feb 21;4(2):100911. PMID: 36657446
Pharmacol Res

Chelidonine selectively inhibits the growth of gefitinib-resistant non-small cell lung cancer cells through the EGFR-AMPK pathway. [Abstract]

2020 Sep;159:104934. PMID: 32464330
Pharmacol Res

Cordycepin Inhibits Drug-resistance Non-small Cell Lung Cancer Progression by Activating AMPK Signaling Pathway. [Abstract]

2019 Jun:144:79-89. PMID: 30974169
Cancer Lett

Identification and characterization of Bufalin as a novel EGFR degrader. [Abstract]

2025 Apr 10:217715. PMID: 40220852
Cell Death Dis

TRIB2 modulates proteasome function to reduce ubiquitin stability and protect liver cancer cells against oxidative stress. [Abstract]

2021 Jan 7;12(1):42. PMID: 33414446
Osteoarthritis Cartilage

Synovial fluid from end-stage osteoarthritis induces proliferation and fibrosis of articular chondrocytes via MAPK and RhoGTPase signaling. [Abstract]

2022 Jun;30(6):862-874. PMID: 35176481
J Pharm Anal

Development of a competitive enzyme-linked immunosorbent assay for therapeutic drug monitoring of afatinib. [Abstract]

2019 Feb;9(1):49-54. PMID: 30740257
Acta Pharmacol Sin

143D, a novel selective KRASG12C inhibitor exhibits potent antitumor activity in preclinical models. [Abstract]

2023 Jul;44(7):1475-1486. PMID: 36725884
EMBO Mol Med

Upfront admixing antibodies and EGFR inhibitors preempts sequential treatments in lung cancer models. [Abstract]

2021 Apr 9;13(4):e13144. PMID: 33660397
NPJ Parkinsons Dis

EGFR phosphorylates DNAJB1 to suppress α-synuclein aggregation in Parkinson's disease. [Abstract]

2025 Jun 7;11(1):157. PMID: 40483356
ACS Appl Mater Interfaces

Intelligent Biomimetic Nanoplatform for Systemic Treatment of Metastatic Triple-Negative Breast Cancer via Enhanced EGFR-Targeted Therapy and Immunotherapy. [Abstract]

2022 May 25;14(20):23152-23163. PMID: 35549005
NPJ Precis Oncol

High-throughput screening identifies NT-1 that synergizes with MRTX1133 against acquired resistant KRASG12D colorectal cancer. [Abstract]

2026 Apr 8;10(1):211. PMID: 41951768
J Transl Med

Combined treatment with inhibitors of ErbB Receptors and Hh signaling pathways is more effective than single treatment in reducing the growth of malignant mesothelioma both in vitro and in vivo. [Abstract]

2022 Jun 25;20(1):286. PMID: 35752861
Oncogene

Suppression of heparan sulfation re-sensitizes YAP1-driven melanoma to MAPK pathway inhibitors. [Abstract]

2022 Aug;41(32):3953-3968. PMID: 35798875
Oncogene

Epigenetic silencing of miR-483-3p promotes acquired gefitinib resistance and EMT in EGFR-mutant NSCLC by targeting integrin β3. [Abstract]

2018 Aug;37(31):4300-4312. PMID: 29717264
Clin Transl Med

Multi-omic profiling defines three distinct molecular subtypes of urothelial carcinoma with implications for precision therapy. [Abstract]

2026 Mar;16(3):e70638. PMID: 41804750
Sci Signal

TSHZ2 is an EGF-regulated tumor suppressor that binds to the cytokinesis regulator PRC1 and inhibits metastasis. [Abstract]

2021 Jun 22;14(688):eabe6156. PMID: 34158398
Acta Neuropathol Commun

Identifying and exploiting combinatorial synthetic lethality by characterizing adaptive kinome rewiring of EGFRvIII-driven glioblastoma. [Abstract]

2025 Jun 28;13(1):143. PMID: 40581663
J Mater Chem B

Overcoming ABCG2-mediated multidrug resistance by a mineralized hyaluronan-drug nanocomplex. [Abstract]

2016 Nov 7;4(41):6652-6661. PMID: 32263520
Mol Cancer Ther

Dual Inhibitors of KRASG12D and HSP90 are Effective Against KRASG12D Inhibitor Resistance. [Abstract]

2025 Oct 23. PMID: 41129140
Pharmaceutics

Drug Repurposing for the Identification of Compounds with Anti-SARS-CoV-2 Capability via Multiple Targets. [Abstract]

2022 Jan 12;14(1):176. PMID: 35057070
Mol Cancer Ther

Afatinib Is a New Therapeutic Approach in Chordoma with a Unique Ability to Target EGFR and Brachyury. [Abstract]

2018 Mar;17(3):603-613. PMID: 29237806

Afatinib dimaleate 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 were resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC₅₀s for each cell line are reported.

Afatinib dimaleate 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 were resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC₅₀s of the different inhibitors are reported.
Cancer Drug Resist

Novel FAK inhibitors suppress tumor growth and reverse EGFR-TKI resistance in non-small cell lung cancer. [Abstract]

2025 Nov 5:8:57. PMID: 41281943
Biol Direct

In vitro synergistic effect of AXL, FAK and ErbB receptors inhibitors for head and neck cancer. [Abstract]

2025 Jul 2;20(1):77. PMID: 40605022
Cancer Nanotechnol

12, 13 (2021).
Int Immunopharmacol

Afatinib inhibits esophageal squamous cell carcinoma by regulating ferroptosis and NRF2 protein homeostasis. [Abstract]

2026 Mar 1:172:116131. PMID: 41520560
Eur J Pharmacol

Discovery of 4-((3,4-dichlorophenyl)amino)-2-methylquinolin-6-ol derivatives as EGFR and HDAC dual inhibitors. [Abstract]

2023 Dec 5:960:176114. PMID: 37863412
Mol Cancer Res

TAS6417/CLN-081 Is a Pan-Mutation-Selective EGFR Tyrosine Kinase Inhibitor with a Broad Spectrum of Preclinical Activity against Clinically Relevant EGFR Mutations. [Abstract]

2019 Nov;17(11):2233-2243. PMID: 31467113
Toxicology

EGFR-TKIs induce acneiform rash and xerosis via Caspase-3/GSDME-mediated pyroptosis of keratinocytes and sebocytes. [Abstract]

2024 Nov 26:154018. PMID: 39608440
Cancers (Basel)

Evaluation of Combined Chemotherapy and Genomic-Driven Targeted Therapy in Patient-Derived Xenografts Identifies New Therapeutic Approaches in Squamous Non-Small-Cell Lung Cancer Patients. [Abstract]

2024 Aug 7;16(16):2785. PMID: 39199558
Cancer Sci

Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. [Abstract]

2018 Apr;109(4):1166-1176. PMID: 29465762

Afatinib dimaleate 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.
Adv Ther

2024 Jul 18.
Sci Rep

A novel human acute myeloid leukemia cell line SDEY-AML1 with KMT2A: MLLT3, IKZF1: EVX1 fusions exhibits high tumorigenicity in NSG mice. [Abstract]

2026 Feb 8;16(1):7792. PMID: 41656387
PLoS Comput Biol

[The epidemiology of arterial hypertension]. [Abstract]

2020 Feb 26;16(2):e1007701. PMID: 2101536
Viruses

Screening and Identification of Lujo Virus Inhibitors Using a Recombinant Reporter Virus Platform. [Abstract]

2021 Jun 28;13(7):1255. PMID: 34203149
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
Cell Biol Int

Sensitization of HT29 colorectal cancer cells to vemurafenib in three-dimensional collagen cultures. [Abstract]

2020 Feb;44(2):621-629. PMID: 31736196
J Pharm Biomed Anal

Comparative studies on the human serum albumin binding of the clinically approved EGFR inhibitors gefitinib, erlotinib, afatinib, osimertinib and the investigational inhibitor KP2187. [Abstract]

2018 May 30:154:321-331. PMID: 29567575
Genes (Basel)

The Impact of Bevacizumab and miR200c on EMT and EGFR-TKI Resistance in EGFR-Mutant Lung Cancer Organoids. [Abstract]

2024 Dec 19;15(12):1624. PMID: 39766891
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
PLoS One

DSE promotes aggressive glioma cell phenotypes by enhancing HB-EGF/ErbB signaling. [Abstract]

2018 Jun 4;13(6):e0198364. PMID: 29864158
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
Int J Radiat Biol

Celecoxib and Afatinib synergistic enhance radiotherapy sensitivity on human non-small cell lung cancer A549 cells. [Abstract]

2021;97(2):170-178. PMID: 33164600
Acta Histochem

Immunohistochemical localization of afatinib in male rat intestines and skin after its oral administration. [Abstract]

2019 Nov;121(8):151439. PMID: 31500866
GEN Biotechnol

2025 Apr 17.
J Oral Biosci

Antihypertensive agent losartan promotes tongue squamous cell carcinoma cell proliferation via EGFR/ERK1/2/cyclin D1 signaling axis. [Abstract]

2024 Sep 6:S1349-0079(24)00198-1. PMID: 39245205
Biochem Biophys Res Commun

2026 Feb 12:800:153165. PMID: 41548485

Afatinib dimaleate purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2026 Feb 12:800:153165.

ActE_21 binding to A549, SK-BR-3 and A431 after incubation with Afatinib (Afatinib dimaleate; 50 nM) for 120 min at 37 °C. Afatinib increases EGF-EGFR complex surface levels in A549 and SK-BR-3 cell.
Oncol Lett

EGFR and ERK activation resists flavonoid quercetin-induced anticancer activities in human cervical cancer cells in vitro. [Abstract]

2021 Nov;22(5):754. PMID: 34539858
Cryobiology

Cryoprotectant toxicity in Caenorhabditis elegans. [Abstract]

2019 Feb:86:71-76. PMID: 30527584
Cell Physiol Biochem

Stimulation of Eryptosis by Afatinib. [Abstract]

2018;47(3):1259-1273. PMID: 29913444
Bioanalysis

Development and validation of an ELISA with high sensitivity for therapeutic monitoring of afatinib. [Abstract]

2018 Sep 1;10(18):1511-1523. PMID: 30117333
Biomed Chromatogr

Simultaneous and rapid determination of gefitinib, erlotinib and afatinib plasma levels using liquid chromatography/tandem mass spectrometry in patients with non-small-cell lung cancer. [Abstract]

2016 Jul;30(7):1150-4. PMID: 26525154
Biol Methods Protoc

Optimizing drug sensitivity assays in patient-derived tumor organoids: a comparison of IC50 estimation methods and experimental parameters. [Abstract]

2025 Feb 13;10(1):bpaf012. PMID: 40060949
Xenobiotica

Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1. [Abstract]

2018 Oct;48(10):1059-1071. PMID: 29034773
bioRxiv

2026 Jun 19.
bioRxiv

2026 Mar 12.
bioRxiv

2026 Jan 9.
bioRxiv

2026 Jan 12.
Technical University of Dresden

2025.
bioRxiv

2025 Dec 5.
bioRxiv

2025 Nov 24.
SSRN

2025 Jul 4.
bioRxiv

Modeling acquired TKI resistance and effective combination therapeutic strategies in murine RET+ lung adenocarcinoma. [Abstract]

2025 Jun 7:2025.06.04.657911. PMID: 40502048
World J Exp Med

Establishment and characterization of a new human gallbladder cancer cell line, OCUG-2. [Abstract]

2025 Jun 20;15(2):100443. PMID: 40546672
State University of New York at Buffalo

2025.
bioRxiv

BRAFV600E-Driven Lung Tumorigenesis Requires Ligand-Mediated Activation of ERBB Receptor Signaling. [Abstract]

2025 May 9:2025.05.04.652129. PMID: 40654950

Afatinib dimaleate purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 May 9:2025.05.04.652129. [Abstract]

Afatinib dimaleate (15 mg/kg; oral gavage; once daily for 8 weeks) reduced tumor burden and tumor diameter in Braf^CAT mice.

Afatinib dimaleate purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 May 9:2025.05.04.652129. [Abstract]

Afatinib dimaleate (Afatinib; 15 mg/kg; oral gavage; once daily for 8 weeks). Immunohistochemistry analyses of phosphorylated ERK (pT202, Y204) in Braf^CAT formalin fixed paraffin embedded (FFPE) mouse lung tissue.

Afatinib dimaleate purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 May 9:2025.05.04.652129. [Abstract]

Afatinib dimaleate (A; 50 nM; 2 or 24 h), alone or in combination with dabrafenib and trametinib (D+T+A), enhances pathway blockade in HCC364 human BRAF^V600E+ lung cancer cells.
Patent

US20240344020A1
Patent

US20240344020A1.
bioRxiv

2024 October 04.
Research Square Preprint

2024 Nov 26.
bioRxiv

2024 Feb 12.
bioRxiv

Structural dynamics of the active HER4 and HER2/HER4 complexes is finely tuned by different growth factors and glycosylation. [Abstract]

2024 Jan 4:2023.10.06.561161. PMID: 38260342
University of Cádiz

2023 Oct.
bioRxiv

2023 Sep 13.
Research Square Print

2023 Jan 6.
bioRxiv

October 28, 2021.
Research Square Preprint

2021 Jul.
Chem Rep

2019, 1(1): 3-12.
Patent

US20190010159A1.
Oncotarget

Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells. [Abstract]

2015 Oct 13;6(31):31313-22. PMID: 26375053
Oncotarget

Afatinib circumvents multidrug resistance via dually inhibiting ATP binding cassette subfamily G member 2 in vitro and in vivo. [Abstract]

2014 Dec 15;5(23):11971-85. PMID: 25436978

Afatinib dimaleate 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.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (139.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (69.63 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.3926 mL

6.9630 mL

13.9260 mL

5 mM

0.2785 mL

1.3926 mL

2.7852 mL

10 mM

0.1393 mL

0.6963 mL

1.3926 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 100 mg/mL (139.26 mM); Clear solution; Need ultrasonic

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (291 KB)
SDS (557 KB)
- English - EN (557 KB)
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- Portuguese - PT (557 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	1.3926 mL	6.9630 mL	13.9260 mL	34.8151 mL
	5 mM	0.2785 mL	1.3926 mL	2.7852 mL	6.9630 mL
	10 mM	0.1393 mL	0.6963 mL	1.3926 mL	3.4815 mL
	15 mM	0.0928 mL	0.4642 mL	0.9284 mL	2.3210 mL
	20 mM	0.0696 mL	0.3482 mL	0.6963 mL	1.7408 mL
	25 mM	0.0557 mL	0.2785 mL	0.5570 mL	1.3926 mL
	30 mM	0.0464 mL	0.2321 mL	0.4642 mL	1.1605 mL
	40 mM	0.0348 mL	0.1741 mL	0.3482 mL	0.8704 mL
	50 mM	0.0279 mL	0.1393 mL	0.2785 mL	0.6963 mL
	60 mM	0.0232 mL	0.1161 mL	0.2321 mL	0.5803 mL
DMSO	80 mM	0.0174 mL	0.0870 mL	0.1741 mL	0.4352 mL
DMSO	100 mM	0.0139 mL	0.0696 mL	0.1393 mL	0.3482 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Afatinib dimaleate

107 Cited Publications

100 mg Obtenir un devis

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