Free shipping on all orders over $ 500


Cat. No. M1913
Neratinib Structure


Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 27  USD30 In stock
10mg USD 45  USD50 In stock
50mg USD 90  USD100 In stock
100mg USD 135  USD150 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

Neratinib is a potent irreversible inhibitor of epidermal growth factor receptor and human epidermal receptor 2 with IC50 of 92 nM and 59 nM, respectively. Neratinib inhibits the proliferation of EGFR-dependent A431 cells with an IC50 of 81 nM. Neratinib (HKI-272) also weakly inhibits tyrosine kinases KDR and Src with IC50 of 0.8 μM and 1.4 μM, respectively. Likewise, Neratinib inhibited the photolabeling of ABCB1 with [(125)I]iodoarylazidoprazosin in a concentration-dependent manner (IC50 = 0.24 μM). Neratinib enhanced the sensitivity of ABCB1-overexpressing cells to ABCB1 substrates. It is noteworthy that Neratinib augmented the effect of chemotherapeutic agents in inhibiting the growth of ABCB1-overexpressing primary leukemia blasts and KBv200 cell xenografts in nude mice. Moreover, Neratinib increased doxorubicin accumulation in ABCB1-overexpressing cell lines and Rhodamine 123 accumulation in ABCB1-overexpressing cell lines and primary leukemia blasts. Neratinib (HKI-272) stimulated the ATPase activity of ABCB1 at low concentrations but inhibited it at high concentrations.

Product Citations
Customer Product Validations & Biological Datas
Source ACS Chem Biol (2016). Figure 5. Neratinib (Abmole Bioscience)
Method FECH inhibition assay
Cell Lines K562 Cells
Concentrations 1 μM
Incubation Time 6 days
Results In line with the Kd values obtained from kinobead experiments, Vemurafenib, CUDC 101, Cyc-116, Linsitinib, MK-2461, Neratinib, GSK-690693, and Crenolanib decreased FECH binding to the PPIX beads by 50% or more compared to the DMSO control.
Source ACS Chem Biol (2016). Figure 4. Neratinib (Abmole Bioscience)
Method FECH inhibition assay
Cell Lines K562 Cells
Concentrations 1 μM
Incubation Time 6 days
Results We then subjected MK-2461, Neratinib, and Linsitinib to the same assay (1 μM for 6 days), and each drug clearly led to reduced heme levels indicating inhibition of FECH activity in K562 cells with Neratinib showing the most potent effect (60% reduction).
Source ACS Chem Biol (2016). Figure 3. Neratinib (Abmole Bioscience)
Method FECH binding
Cell Lines K562 Cells
Incubation Time
Results The basis of this assay is that proteins bound to a drug molecule are stabilized against heat induced unfolding and aggregation, and the extent of this protection is dose dependent.
Source ACS Chem Biol (2016). Figure 2. Neratinib (Abmole Bioscience)
Method FECH binding
Cell Lines
Incubation Time
Results Figure 2b−f show the full dose response data for five selected inhibitors, and the complete set of these plots can be found in Supporting Information Figure S1 and Table S1.
Cell Experiment
Cell lines 3T3, 3T3/neu, A431, SK-Br-3, BT474, MDA-MB-435, and SW62 cells
Preparation method Cell Proliferation Assays.
Cells were plated in 96-well tissue culture plates (3T3, 3T3/neu, 5000 cells/well; A431, SK-Br-3, BT474, MDA-MB-435, and SW620, 10,000 cells/well). The following day, dilutions of compound (0.5 ng/ml–5 μg/ml) were added, and cells were cultured for 2 days (6 days for BT474). Cell proliferation was determined using sulforhodamine B, a protein binding dye. Briefly, cells were fixed with 10% trichloroacetic acid and washed extensively with water. Cells were then stained with 0.1% sulforhodamine B (Sigma-Aldrich) and washed in 5% acetic acid. Protein-associated dye was solubilized in 10 mm Tris, and absorbance was measured at 450 nm (Victor2). Inhibition of cell proliferation was calculated using the formula: percentage of inhibition = 100 − 100 (Td − To/Tc − To), where Td is the absorbance of drug treated cells, Tc is the absorbance of untreated cells, and To is the absorbance at the time of drug addition. To values were determined by plating cells separately and fixing them at the time of drug addition. The concentration of compound which inhibits cell proliferation by 50% (IC50) was determined from inhibition curves.
Concentrations 0.5 ng/ml-5 μg/ml
Incubation time 2 days
Animal Experiment
Animal models BT474, MCF-7, and SK-OV-3 tumour xenografts model in female athymic (nude) mice
Formulation 0.5% methocellulose-0.4% polysorbate-80 (Tween 80)
Dosages 40 or 60mg/kg daily for 20 days
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 557.04
Formula C30H29ClN6O3
CAS Number 698387-09-6
Purity 99.88%
Solubility DMSO 8 mg/mL
Storage at -20°C

Neratinib reverses ATP-binding cassette B1-mediated chemotherapeutic drug resistance in vitro, in vivo, and ex vivo.
Zhao XQ, et al. Mol Pharmacol. 2012 Jul;82(1):47-58. PMID: 22491935.

Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase.
Rabindran SK, et al. Cancer Res. 2004 Jun 1;64(11):3958-65. PMID: 15173008.

Related EGFR/HER2 Products

TX1-85-1 is an ErbB3 inhibitor with IC50 of 23 nM, it is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3.

AZD3759 hydrochloride

AZD3759 hydrochloride is an orally available inhibitor of the epidermal growth factor receptor (EGFR) with potential antineoplastic activity.

Avitinib (AC0010)

Avitinib (Abivertinib; AC0010) is a third-generation irreversible EGFR tyrosine kinase inhibitor, with potential antineoplastic activity.

Irbinitinib (Tucatinib)

Tucatinib, also known as Irbinitinib and ONT-380, is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (HER2).


Lazertinib, also known as YH-25448 and GNS-1480, is an oral active, highly potent, mutant-selective and irreversible EGFR Tyrosine-kinase inhibitors (TKIs) targets both the T790M mutation and activating EGFR mutations while sparing wild type-EGFR.

Abmole Inhibitor Catalog 2017

Keywords: Neratinib, HKI-272 supplier, EGFR/HER2, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.