Cat. No.: HY-32721

Neratinib

(Synonyms: HKI-272)

27 Cited Publications

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Based on 27 publication(s) in Google Scholar

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

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

Pureté: 99.94%
CAS No.: 698387-09-6
Formule: C₃₀H₂₉ClN₆O₃
Masse moléculaire:557.04

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Neratinib Chemical Structure

CAS No.: 698387-09-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (27)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
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Activité biologique

Description

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

IC₅₀ & Target^[1]

HER2

59 nM (IC₅₀)

EGFR

92 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	EC₅₀	81 nM Compound: 4, HKI-272	Inhibition of human Her2 in A431 cells Inhibition of human Her2 in A431 cells	[PMID: 18077425]
A-431	IC₅₀	0.086 μM Compound: 25o (table 3)	Inhibition of human A431 cell proliferation Inhibition of human A431 cell proliferation	[PMID: 15715478]
A-431	IC₅₀	2.15 μM Compound: Neratinib	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition Antiproliferative activity against human A-431 cells assessed as cell growth inhibition	[PMID: 34749202]
BaF3	GI₅₀	1.9 μM Compound: 2; HKI272	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
BaF3	IC₅₀	<1 nM Compound: HKI-272	Antiproliferative activity against mouse BaF3 cells harboring ERBB2 Ins 774YVMA mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring ERBB2 Ins 774YVMA mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	<1 nM Compound: HKI-272	Antiproliferative activity against mouse BaF3 cells harboring ERBB2 Ins G776V,C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring ERBB2 Ins G776V,C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	<1 nM Compound: HKI-272	Antiproliferative activity against mouse BaF3 cells harboring wildtype ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring wildtype ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	1.25 μM Compound: HKI-272	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	108 nM Compound: HKI-272	Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	14.59 nM Compound: Neratinib	Antiproliferative activity against mouse BaF3 cells harboring HER2 YVMA mutant by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring HER2 YVMA mutant by CellTiter-Glo assay	[PMID: 38518121]
BaF3	IC₅₀	16 nM Compound: HKI-272	Antiproliferative activity against mouse BaF3 cells harboring EGFR vIII mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR vIII mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	180 nM Compound: 8, HKI-272	Cytotoxicity against mouse BA/F3 cells expressing EGFR L858R/T790M mutant Cytotoxicity against mouse BA/F3 cells expressing EGFR L858R/T790M mutant	[PMID: 19239229]
BaF3	IC₅₀	2.17 μM Compound: HKI-272	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	2.27 μM Compound: HKI-272	Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	2.37 μM Compound: HKI-272	Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	265 nM Compound: HKI-272	Antiproliferative activity against mouse BaF3 cells harboring EGFR A767_V769dupASV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR A767_V769dupASV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	3 nM Compound: HKI-272	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	3.5 nM Compound: 8, HKI-272	Cytotoxicity against mouse BA/F3 cells expressing EGFR L858R mutant Cytotoxicity against mouse BA/F3 cells expressing EGFR L858R mutant	[PMID: 19239229]
BT-474	EC₅₀	2 nM Compound: 4, HKI-272	Inhibition of human Her2 in BT474 cells Inhibition of human Her2 in BT474 cells	[PMID: 18077425]
BT-474	IC₅₀	10 nM Compound: Neratinib	Antiproliferative activity against human BT-474 cells by CellTiter-Glo assay Antiproliferative activity against human BT-474 cells by CellTiter-Glo assay	[PMID: 38518121]
BT-474	IC₅₀	2.06 nM Compound: Neratinib	Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
Calu-3	IC₅₀	54 nM Compound: HKI-272	Antiproliferative activity against human Calu-3 cells harboring ERBB2 amp mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human Calu-3 cells harboring ERBB2 amp mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
COLO-678	IC₅₀	694.11 nM Compound: Neratinib	Antiproliferative activity against human COLO-678 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human COLO-678 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
ES-2	IC₅₀	787.91 nM Compound: Neratinib	Antiproliferative activity against human ES2 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human ES2 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
HBL-100	GI₅₀	1.6 μM Compound: 1	Growth inhibition of human HBL-100 cells Growth inhibition of human HBL-100 cells	[PMID: 38870832]
HCC827	IC₅₀	94 nM Compound: HKI-272	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
MDA-MB-468	IC₅₀	405.51 nM Compound: Neratinib	Antiproliferative activity against human MDA-MB-468 cells overexpressing wild type EGFR assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MDA-MB-468 cells overexpressing wild type EGFR assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
MFE-280	IC₅₀	1291.95 nM Compound: Neratinib	Antiproliferative activity against human MFE-280 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MFE-280 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
NCI-H1975	IC₅₀	153 nM Compound: HKI-272	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
NCI-H3255	IC₅₀	55 nM Compound: HKI-272	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
NCI-H441	IC₅₀	1280.72 nM Compound: Neratinib	Antiproliferative activity against human NCI-H441 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human NCI-H441 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
NCI-N87	IC₅₀	0.64 nM Compound: Neratinib	Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
NCI-N87	IC₅₀	7.73 nM Compound: Neratinib	Antiproliferative activity against human NCI-N87 cells by CellTiter-Glo assay Antiproliferative activity against human NCI-N87 cells by CellTiter-Glo assay	[PMID: 38518121]
NUGC-4	IC₅₀	38.15 nM Compound: Neratinib	Antiproliferative activity against human NUGC-4 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human NUGC-4 cells assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
PC-9	IC₅₀	96 nM Compound: HKI-272	Antiproliferative activity against human PC-9 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human PC-9 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
Sf9	IC₅₀	2.5 nM Compound: 3, HKI-272	Inhibition of human wild type EGFR expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting Inhibition of human wild type EGFR expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting	[PMID: 24900643]
Sf9	IC₅₀	66 nM Compound: 3, HKI-272	Inhibition of human EGFR T790M/L858R mutant expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting Inhibition of human EGFR T790M/L858R mutant expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting	[PMID: 24900643]
SK-BR-3	EC₅₀	2 nM Compound: 4, HKI-272	Inhibition of human Her2 in SKBR3 cells Inhibition of human Her2 in SKBR3 cells	[PMID: 18077425]
SK-BR-3	IC₅₀	0.0018 μM Compound: 25o (table 3)	Inhibition of human SKBr3 cell proliferation Inhibition of human SKBr3 cell proliferation	[PMID: 15715478]
SK-BR-3	IC₅₀	10.34 nM Compound: Neratinib	Antiproliferative activity against human SK-BR-3 cells overexpressing wild type HER2 assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay Antiproliferative activity against human SK-BR-3 cells overexpressing wild type HER2 assessed as cell growth inhibition incubated for 72 hrs by Celltiter-Glo assay	[PMID: 35319895]
SK-BR-3	IC₅₀	3.97 μM Compound: Neratinib	Antiproliferative activity against human SK-BR-3 cells assessed as cell growth inhibition Antiproliferative activity against human SK-BR-3 cells assessed as cell growth inhibition	[PMID: 34749202]
SK-BR-3	IC₅₀	7.2 nM Compound: 45	Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by sulforhodamine B colorimetric assay Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by sulforhodamine B colorimetric assay	[PMID: 36332549]
SW-620	EC₅₀	690 nM Compound: 4, HKI-272	Inhibition of human Her2 in SW620 cells Inhibition of human Her2 in SW620 cells	[PMID: 18077425]
SW-620	IC₅₀	0.73 μM Compound: 25o (table 3)	Inhibition of human SW620 cell proliferation Inhibition of human SW620 cell proliferation	[PMID: 15715478]

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 698387-09-6
Appearance Solid
Masse moléculaire 557.04
Formule C₃₀H₂₉ClN₆O₃
Color White to yellow
SMILES

ClC1=C(OCC2=NC=CC=C2)C=CC(NC3=C(C#N)C=NC4=CC(OCC)=C(NC(/C=C/CN(C)C)=O)C=C43)=C1
Synonyms

HKI-272
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

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 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 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 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
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 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.
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 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 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 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 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
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
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
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
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
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 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
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
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
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

Solvant et solubilité

In Vitro:

DMSO : 8.33 mg/mL (14.95 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

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7952 mL

8.9760 mL

17.9520 mL

5 mM

0.3590 mL

1.7952 mL

3.5904 mL

10 mM

0.1795 mL

0.8976 mL

1.7952 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.83 mg/mL (1.49 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
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Instruction de manipulation (2659 KB)

Références

[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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7952 mL	8.9760 mL	17.9520 mL	44.8801 mL
	5 mM	0.3590 mL	1.7952 mL	3.5904 mL	8.9760 mL
	10 mM	0.1795 mL	0.8976 mL	1.7952 mL	4.4880 mL

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