Cat. No.: HY-32721B

Neratinib maleate

(Synonyms: HKI-272 maleate)

27 Cited Publications

Customer Review

Based on 27 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.

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

Purity: 99.74%
CAS No.: 915942-22-2
Formula: C₃₄H₃₃ClN₆O₇
Molecular Weight:673.11

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Neratinib maleate Chemical Structure

CAS No.: 915942-22-2

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (27)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC₅₀s of 59 nM and 92 nM, respectively^[1].

IC₅₀ & Target

HER2

59 nM (IC₅₀)

EGFR

92 nM (IC₅₀)

All EGFR Isoforms :

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.

Cell Proliferation Assay^[1]

Cell Line:

3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620
Concentration:

0.5 ng/mL–5 μg/mL
Incubation Time:

2 days (6 days for BT474)
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.

Western Blot Analysis^[1]

Cell Line:

BT474 or A431 cells
Concentration:

0, 2, 10, 50, 100 and 200 nM
Incubation Time:

3 h
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.

Cell Cycle Analysis^[1]

Cell Line:

BT474
Concentration:

0–2 nM
Incubation Time:

12–16 h
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

Neratinib (HKI-272) (0-80 mg/kg/day; i.g.; 42 days) shows anticancer activities against cancer cells that expresses high levels of HER-2 or EGFR^[1].

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

Animal Model:

Female athymic (nude) mice, tumor xenograft^[1]
Dosage:

10, 20, 40, 60 or 80 mg/kg/day
Administration:

Gavage, 42 days
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

CAS No. 915942-22-2
Appearance Solid
Molecular Weight 673.11
Formula C₃₄H₃₃ClN₆O₇
Color White to off-white
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
Synonyms

HKI-272 maleate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (27)

All Cell Proliferation/Viability AssayIn Vivo Efficacy StudyWBFlow CytometryHistological Imaging/StainingOthers

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Journal Impact Factor

Nature

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

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).
Cancer Cell

EGFR-activated myofibroblasts promote metastasis of pancreatic cancer. [Abstract]

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

TRIM24-RIP3 axis perturbation accelerates osteoarthritis pathogenesis. [Abstract]

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

The ERBB network facilitates KRAS-driven lung tumorigenesis. [Abstract]

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.
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.
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.
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

Disabled 1 Is Part of a Signaling Pathway Activated by Epidermal Growth Factor Receptor. [Abstract]

2021 Feb 9;22(4):1745. PMID: 33572344
Cancer Sci

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

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.
J Biol Chem

Activation of Gcn2 by small molecules designed to be inhibitors. [Abstract]

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

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

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
bioRxiv

2026 Jun 19.
Res Sq

2026 Mar 10.
Cornell University

2025.
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

Solvent & Solubility

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)

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

1.4856 mL

7.4282 mL

14.8564 mL

5 mM

0.2971 mL

1.4856 mL

2.9713 mL

10 mM

0.1486 mL

0.7428 mL

1.4856 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 (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.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
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)
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)
Handling Instructions (2659 KB)

References

[1]. Rabindran SK, et al. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res, 2004, 64(11), 3958-3965. [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
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

Keywords

Neratinib maleate

27 Cited Publications

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Neratinib maleate

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Publications Citing Use of MedChemExpress (MCE) Neratinib maleate

All EGFR Isoforms

Biological Activity

Chemical Information

Publications (27)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Neratinib maleate Related Classifications

HY-32721B Related Classifications