Neratinib maleate
Based on 28 publication(s) in Google Scholar
Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively.
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- Purity : 99.74%
- CAS No.: 915942-22-2
- 화학식: C34H33ClN6O7
- 분자량:673.11
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Neratinib maleate
More- Nature. 2026 Jan;649(8098):1032-1041. [Abstract]
- Cancer Cell. 2024 Jan 8;42(1):101-118.e11. [Abstract]
- Cancer Discov. 2026 Apr 2. [Abstract]
- Ann Rheum Dis. 2020 Dec;79(12):1635-1643. [Abstract]
- Nat Commun. 2023 Nov 2;14(1):6997. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Sci Transl Med. 2018 Jun 20;10(446):eaao2565. [Abstract]
- NPJ Precis Oncol. 2026 Apr 8;10(1):211. [Abstract]
- J Transl Med. 2023 Sep 9;21(1):611. [Abstract]
- Oncogene. 2021 Nov;40(44):6273-6283. [Abstract]
- Clin Transl Med. 2026 Mar;16(3):e70638. [Abstract]
- Cell Rep. 2022 Apr 5;39(1):110595. [Abstract]
- Cell Syst. 2019 Jul 24;9(1):35-48.e5. [Abstract]
- Pharmaceutics. 2022 Jan 12;14(1):176. [Abstract]
- Mol Cancer Ther. 2018 Mar;17(3):603-613. [Abstract]
- Acta Neuropathol Commun. 2025 Jun 28;13(1):143. [Abstract]
- Int J Mol Sci. 2021 Feb 9;22(4):1745. [Abstract]
- Cancer Sci. 2018 Apr;109(4):1166-1176. [Abstract]
- J Biol Chem. 2023 Apr;299(4):104595 [Abstract]
- Breast Cancer (Dove Med Press). 2023 Nov 6:15:785-799. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Open Life Sci. 2023 Jan 10;18(1):20220535. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- Biomed Pharmacother. 2026 Sep:202:119803.
- bioRxiv. 2026 Jun 19.
- Res Sq. 2026 Mar 10.
- Cornell University. 2025.
- bioRxiv. 2024 Dec 20:2024.12.19.629301. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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Flow Cytometry
All EGFR Isoforms
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Biological Activity
제품 설명
IC50 & Target
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HER2 59 nM (IC50) |
EGFR 92 nM (IC50) |
In Vitro
Neratinib displays no activity against other serine-threonine kinases such as Akt, cyclin D1/cdk4, cyclin E/cdk2, cyclin B1/cdk1, IKK-2, MK-2, PDK1, c-Raf, and Tpl-2, as well as the tyrosine kinase c-Met[1].
Neratinib (0.5 ng/mL–5 μg/mL, 2 days) inhibits the proliferation of cell lines that show high levels of HER-2 (3T3/neu, SK-Br-3, and BT474) and is much less active in cell lines that express neither HER-2 nor EGFR (3T3, MDA-MB-435, and SW620) [1].
Neratinib (0-2 nM, 12-16 h) arrests BT474 cell cycle at G1-S phase[1].
Neratinib results in the inhibition of MAPK and Akt phosphorylation, down-regulation of cyclin D1 levels, and induction of p27[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620
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Concentration:0.5 ng/mL–5 μg/mL
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Incubation Time:2 days (6 days for BT474)
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Result:Inhibited cell proliferation with IC50 values of 700 ± 78, 3 ± 0.14, 2 ± 0.18, 2 ± 0.06, 81± 9, 960 ± 165 and 690 ± 84 nM against 3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620 cells, respectively.
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Cell Line:BT474 or A431 cells
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Concentration:0, 2, 10, 50, 100 and 200 nM
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Incubation Time:3 h
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Result:Decreased ligand-independent receptor phosphorylation by 50% (IC50) at 5 nM in BT474 cells, repressed EGF-dependent phosphorylation of EGFR in A431 cells at a comparable dose (IC50 = 3 nM).
Effectively repressed phosphorylation of MAPK and Akt in BT474 cells.
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Cell Line:BT474
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Concentration:0–2 nM
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Incubation Time:12–16 h
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Result:Blocked cell cycle progression, causing a G1-S arrest, a 50% decrease in the number of cells in the S (DNA synthesis) phase of the cell cycle was observed at a concentration of 2 nM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic (nude) mice, tumor xenograft[1]
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Dosage:10, 20, 40, 60 or 80 mg/kg/day
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Administration:Gavage, 42 days
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Result:Reduced tumor growth in a dose-dependent manner in 3T3/neu, BT474, SK-OV-3 and A431 xenografts, but was o inactive in xenografts of MX-1 and MCF-7. Inhibited phosphorylation of HER-2 in BT474 xenografts.
Chemical Information
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CAS No. 915942-22-2
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Appearance Solid
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분자량 673.11
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화학식 C34H33ClN6O7
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Color White to off-white
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SMILES
OC(/C=C\C(O)=O)=O.CCOC(C(NC(/C=C/CN(C)C)=O)=C1)=CC2=C1C(NC3=CC(Cl)=C(C=C3)OCC4=CC=CC=N4)=C(C#N)C=N2
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Synonyms
HKI-272 maleate
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (28)
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Journal Impact Factor
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Most Recent
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Nature
2026 Jan;649(8098):1032-1041. PMID: 41299171
Neratinib maleate 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).
Neratinib maleate 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).
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Cancer Cell
2024 Jan 8;42(1):101-118.e11. PMID: 38157863 -
Cancer Discov
HER2 heterogeneous breast cancer models reveal novel therapeutic targets and subclonal dynamics during evolution to resistance to HER2-targeted therapies. [Abstract]2026 Apr 2. PMID: 41925564 -
Ann Rheum Dis
2020 Dec;79(12):1635-1643. PMID: 32895234 -
Nat Commun
Toxic PARP trapping upon cAMP-induced DNA damage reinstates the efficacy of endocrine therapy and CDK4/6 inhibitors in treatment-refractory ER+ breast cancer. [Abstract]2023 Nov 2;14(1):6997. PMID: 37914699 -
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 -
Sci Transl Med
2018 Jun 20;10(446):eaao2565. PMID: 29925636
Neratinib maleate purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2018 Jun 20;10(446):eaao2565. [Abstract]
Immunoblots of 3 individual KM tumors from mice treated for 3 days with Neratinib or vehicle control.
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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
Establishment of a high-fidelity patient-derived xenograft model for cervical cancer enables the evaluation of patient's response to conventional and novel therapies. [Abstract]2023 Sep 9;21(1):611. PMID: 37689699
Neratinib maleate purchased from MedChemExpress. Usage Cited in: J Transl Med. 2023 Sep 9;21(1):611. [Abstract]
Neratinib (48 h) sensitivity of PDXO from patient CAT061 was determined. The average half-maximal inhibitory concentration from three separate experiments (n = 3) for CAT061 PDXO was 40.91 nM.
Neratinib maleate purchased from MedChemExpress. Usage Cited in: J Transl Med. 2023 Sep 9;21(1):611. [Abstract]
Neratinib, 20 mg/kg, was administered five times a week via oral gavage for 20 days. The PDX tumor size of these mice was shown in the left graph, and the weights of the PDX tumors (day 28) were shown in the right graph.
Neratinib maleate purchased from MedChemExpress. Usage Cited in: J Transl Med. 2023 Sep 9;21(1):611. [Abstract]
Neratinib, 20 mg/kg, was administered five times a week via oral gavage for 20 days. Granzyme B (GrzB) expression in CD4+ T cells was determined by flow cytometry (Student's t-test).
Neratinib maleate purchased from MedChemExpress. Usage Cited in: J Transl Med. 2023 Sep 9;21(1):611. [Abstract]
Representative hematoxylin and eosin-stained sections and immunohistochemistry images of Ki67 staining of tumors from each of the treatment groups (scale bar, 50 μm) were shown. Neratinib, 20 mg/kg, was administered five times a week via oral gavage for 20 days.
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Oncogene
Melatonin potentiates the cytotoxic effect of Neratinib in HER2+ breast cancer through promoting endocytosis and lysosomal degradation of HER2. [Abstract]2021 Nov;40(44):6273-6283. PMID: 34556812 -
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 -
Cell Rep
Mesenchymal and stem-like prostate cancer linked to therapy-induced lineage plasticity and metastasis. [Abstract]2022 Apr 5;39(1):110595. PMID: 35385726 -
Cell Syst
A Multi-center Study on the Reproducibility of Drug-Response Assays in Mammalian Cell Lines. [Abstract]2019 Jul 24;9(1):35-48.e5. PMID: 31302153
Neratinib maleate purchased from MedChemExpress. Usage Cited in: Cell Syst. 2019 Jul 24;9(1):35-48.e5. [Abstract]
The results of cell counting for MCF 10A cells treated with Dasatinib or Neratinib (72 h) using two different image processing algorithms included in the Columbus image analysis software package were obtained.
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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 -
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 -
Int J Mol Sci
2021 Feb 9;22(4):1745. PMID: 33572344 -
Cancer Sci
2018 Apr;109(4):1166-1176. PMID: 29465762
Neratinib maleate purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Apr;109(4):1166-1176. [Abstract]
Influence of BIBW 2992 or Neratinib on human epidermal growth factor receptor 2 (HER2) and the downsignal pathway in gastric cancer cell lines.
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J Biol Chem
2023 Apr;299(4):104595 PMID: 36898579 -
Breast Cancer (Dove Med Press)
Therapeutic Advantage of Targeting PRMT5 in Combination with Chemotherapies or EGFR/HER2 Inhibitors in Triple-Negative Breast Cancers. [Abstract]2023 Nov 6:15:785-799. PMID: 37954171 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
Open Life Sci
Systemic investigation of inetetamab in combination with small molecules to treat HER2-overexpressing breast and gastric cancers. [Abstract]2023 Jan 10;18(1):20220535. PMID: 36694697 -
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 -
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bioRxiv
BRAFV600 and ErbB inhibitors directly activate GCN2 in an off-target manner to limit cancer cell proliferation. [Abstract]2024 Dec 20:2024.12.19.629301. PMID: 39763857
용액&용해도
In Vitro:
DMSO : 250 mg/mL (371.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.4856 mL | 7.4282 mL | 14.8564 mL | 37.1410 mL |
| 5 mM | 0.2971 mL | 1.4856 mL | 2.9713 mL | 7.4282 mL | |
| 10 mM | 0.1486 mL | 0.7428 mL | 1.4856 mL | 3.7141 mL | |
| 15 mM | 0.0990 mL | 0.4952 mL | 0.9904 mL | 2.4761 mL | |
| 20 mM | 0.0743 mL | 0.3714 mL | 0.7428 mL | 1.8571 mL | |
| 25 mM | 0.0594 mL | 0.2971 mL | 0.5943 mL | 1.4856 mL | |
| 30 mM | 0.0495 mL | 0.2476 mL | 0.4952 mL | 1.2380 mL | |
| 40 mM | 0.0371 mL | 0.1857 mL | 0.3714 mL | 0.9285 mL | |
| 50 mM | 0.0297 mL | 0.1486 mL | 0.2971 mL | 0.7428 mL | |
| 60 mM | 0.0248 mL | 0.1238 mL | 0.2476 mL | 0.6190 mL | |
| 80 mM | 0.0186 mL | 0.0929 mL | 0.1857 mL | 0.4643 mL | |
| 100 mM | 0.0149 mL | 0.0743 mL | 0.1486 mL | 0.3714 mL |
Neratinib maleate Related Classifications
HY-32721B Related Classifications
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