Neratinib (Synonyms: HKI-272)

Name: Neratinib
Brand: MedChemExpress
SKU: HY-32721
Rating: 5.0 (24 reviews)

Art. -Nr.: HY-32721 Reinheit: 99.94%: Data Sheet
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Neratinib (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC₅₀s of 59 nM and 92 nM, respectively.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr. : 698387-09-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
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10 mg	Auf Lager	Estimated Time of Arrival: December 31
25 mg	Auf Lager	Estimated Time of Arrival: December 31
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Based on 24 publication(s) in Google Scholar

Other Forms of Neratinib:

Neratinib maleate In-stock
Neratinib (Standard) In-stock
Neratinib-d₆ Angebot einholen

24 Publications Citing Use of MCE Neratinib

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

Flow Cytometry

Histological Imaging/Staining

Others

: 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).

: 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.

: 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.

: 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.

: 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.

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle EGFR Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biologische Aktivität
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Beschreibung

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)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	1.9 3 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]
A-431	IC₅₀	2.15 3 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]
A-431	EC₅₀	81 1 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 3 Compound: 25o (table 3)	Inhibition of human A431 cell proliferation Inhibition of human A431 cell proliferation	[PMID: 15715478]
A-431	IC₅₀	0.086 3 Compound: 25o (table 3)	Inhibition of human A431 cell proliferation Inhibition of human A431 cell proliferation	[PMID: 15715478]
BT-474	IC₅₀	2.06 1 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]
BaF3	GI₅₀	1.9 3 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]
COLO-678	IC₅₀	694.11 1 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]
A-431	IC₅₀	2.15 3 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]
NCI-N87	IC₅₀	0.64 1 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]
ES-2	IC₅₀	787.91 1 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]
MDA-MB-468	IC₅₀	405.51 1 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]
BT-474	EC₅₀	2 1 Compound: 4, HKI-272	Inhibition of human Her2 in BT474 cells Inhibition of human Her2 in BT474 cells	[PMID: 18077425]
BT-474	EC₅₀	2 1 Compound: 4, HKI-272	Inhibition of human Her2 in BT474 cells Inhibition of human Her2 in BT474 cells	[PMID: 18077425]
SK-BR-3	EC₅₀	2 1 Compound: 4, HKI-272	Inhibition of human Her2 in SKBR3 cells Inhibition of human Her2 in SKBR3 cells	[PMID: 18077425]
MFE-280	IC₅₀	1291.95 1 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]
BT-474	IC₅₀	10 1 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 1 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]
NCI-H441	IC₅₀	1280.72 1 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]
BT-474	IC₅₀	2.06 1 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]
Sf9	IC₅₀	2.5 1 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]
NCI-N87	IC₅₀	0.64 1 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]
BaF3	IC₅₀	3.5 1 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]
NUGC-4	IC₅₀	38.15 1 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]
BaF3	GI₅₀	1.9 3 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	1.25 3 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]
SK-BR-3	IC₅₀	7.2 1 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]
Sf9	IC₅₀	2.5 1 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]
SK-BR-3	IC₅₀	10.34 1 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]
Sf9	IC₅₀	66 1 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]
BaF3	IC₅₀	108 1 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]
NUGC-4	IC₅₀	38.15 1 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]
SK-BR-3	IC₅₀	10.34 1 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]
BaF3	IC₅₀	14.59 1 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]
SK-BR-3	IC₅₀	7.2 1 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]
BaF3	IC₅₀	16 1 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]
Sf9	IC₅₀	66 1 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]
A-431	EC₅₀	81 1 Compound: 4, HKI-272	Inhibition of human Her2 in A431 cells Inhibition of human Her2 in A431 cells	[PMID: 18077425]
BaF3	IC₅₀	180 1 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 3 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	180 1 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]
MDA-MB-468	IC₅₀	405.51 1 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]
BaF3	IC₅₀	2.27 3 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]
SW-620	EC₅₀	690 1 Compound: 4, HKI-272	Inhibition of human Her2 in SW620 cells Inhibition of human Her2 in SW620 cells	[PMID: 18077425]
BaF3	IC₅₀	2.37 3 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 1 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]
COLO-678	IC₅₀	694.11 1 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 1 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]
BaF3	IC₅₀	3 1 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]
NCI-H441	IC₅₀	1280.72 1 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]
BaF3	IC₅₀	3.5 1 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]
BaF3	IC₅₀	< 1 1 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]
MFE-280	IC₅₀	1291.95 1 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]
BaF3	IC₅₀	< 1 1 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]
SK-BR-3	IC₅₀	3.97 3 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	0.0018 3 Compound: 25o (table 3)	Inhibition of human SKBr3 cell proliferation Inhibition of human SKBr3 cell proliferation	[PMID: 15715478]
BaF3	IC₅₀	< 1 1 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]
SW-620	IC₅₀	0.73 3 Compound: 25o (table 3)	Inhibition of human SW620 cell proliferation Inhibition of human SW620 cell proliferation	[PMID: 15715478]
COLO-678	IC₅₀	694.11 1 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]
Calu-3	IC₅₀	54 1 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]
ES-2	IC₅₀	787.91 1 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 3 Compound: 1	Growth inhibition of human HBL-100 cells Growth inhibition of human HBL-100 cells	[PMID: 38870832]
HCC827	IC₅₀	94 1 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 1 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 1 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 1 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 1 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 1 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 1 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 1 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 1 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 1 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]
SK-BR-3	EC₅₀	2 1 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 3 Compound: 25o (table 3)	Inhibition of human SKBr3 cell proliferation Inhibition of human SKBr3 cell proliferation	[PMID: 15715478]
SK-BR-3	IC₅₀	10.34 1 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 3 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 1 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 1 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 3 Compound: 25o (table 3)	Inhibition of human SW620 cell proliferation Inhibition of human SW620 cell proliferation	[PMID: 15715478]
Sf9	IC₅₀	2.5 1 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 1 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]

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.

Klinische Studie

Molekulargewicht

557.04

Formel

C₃₀H₂₉ClN₆O₃

CAS. Nr.

698387-09-6

Appearance

Solid

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

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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, 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.

Molaritätsrechner
Verdünnungsrechner

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Reinheit & Dokumentation

Purity: 99.94%

Select Batch:

Data Sheet (277 KB) SDS (394 KB)

COA (247 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

Verweise

[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]

Complete Stock Solution Preparation Table

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

Neratinib Related Classifications

Help & FAQs

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

Keywords:

Neratinib698387-09-6HKI-272HKI272HKI 272EGFREpidermal growth factor receptorErbB-1HER1breast cancersolid tumorsnon–small-cell lung cancerBT474A431gastric cancerInhibitorinhibitorinhibit

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Neratinib (Synonyms: HKI-272)

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Neratinib Related Antibodies

24 Publications Citing Use of MCE Neratinib

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Neratinib Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

Neratinib Related Classifications

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