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Neratinib (HKI-272)
Catalog No.S2150
For research use only.
Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.
CAS No. 698387-09-6
Selleck's Neratinib (HKI-272) has been cited by 82 publications
Purity & Quality Control
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Biological Activity
| Description | Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| In vitro |
Neratinib weakly inhibits tyrosine kinases KDR and Src with IC50 of 0.8 μM and 1.4 μM, respectively, being 14- and 24-fold less active compared with HER2. 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. Neratinib selectively inhibits the proliferation of 3T3 cells transfected with the HER2 (3T3/neu), as well as two other HER-2-overexpressing SK-Br-3 and BT474 cells with IC50 values of 2-3 nM, displaying >230-fold potency compared with non-transfected 3T3 cells as well as MDA-MB-435 and SW620 which are EGFR- and HER2-negative. Neratinib also inhibits the proliferation of EGFR-dependent A431 cells with an IC50 of 81 nM. Neratinib reduces HER2 receptor autophosphorylation in BT474 cells with an IC50 of 5 nM, and EGF-dependent phosphorylation of EGFR in A431 cells with IC50 of 3 nM. Blocking of HER-2 by Neratinib results in inhibition of downstream MAPK and Akt pathways with IC50 of 2 nM, more potently than Trastuzumab. Neratinib inhibits the cyclin D1 expression and the phosphorylation of the Rb-susceptibility gene production in BT474 cells with IC50 of 9 nM, leading to G1-S arrest and ultimately decreased cell proliferation. [1] |
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| Cell Data |
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| Assay |
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| In vivo | Oral administration of Neratinib significantly inhibits the growth of 3T3/neu xenografts, with inhibition of 34%, 53%, 98%, and 98% at dose of 10, 20, 40, and 80 mg/kg/day, respectively. Consistent with the inhibition of HER-2 phosphorylation by 84% within 1 hour of administration at 40 mg/kg/day, Neratinib inhibits the growth of BT474 xenografts by 70-82%, 67%, and 93% at dose of 5, 10, and 40 mg/kg/day, respectively. Neratinib is also effective against SK-OV-3 xenografts with inhibition of 31% and 85% at 5 and 60 mg/kg/day, respectively. Neratinib is less potent against EGFR-dependent A431 xenografts than HER-2-dependent tumors, with 32% and 44% inhibition at 5 and 20 mg/kg/day, respectively. Neratinib displays little activity against MCF-7 and MX-1 xenografts expressing low levels of HER-2 and EGFR, with only 28% inhibition at 80 mg/kg/day, suggesting that Neratinib has selective activity for cells expressing HER-2 or EGFR. [1] |
Protocol (from reference)
| Kinase Assay:[1] |
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| Cell Research:[1] |
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| Animal Research:[1] |
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Solubility (25°C)
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In vitro |
DMSO |
5 mg/mL
warmed (8.97 mM) |
| Water |
Insoluble
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| Ethanol |
Insoluble
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In vivo |
Add solvents to the product individually and in order |
5 mg/mL |
Chemical Information
| Molecular Weight | 557.04 | ||
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| Formula | C30H29ClN6O3 |
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| CAS No. | 698387-09-6 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)C=CCN(C)C | ||
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04856475 | Withdrawn | Drug: Neratinib | Breast Cancer|Brain Metastases | Jules Bordet Institute | November 24 2021 | Phase 2 |
| NCT04781374 | Recruiting | Drug: Neratinib | Metastatic Prostate Adenocarcinoma|Castration-resistant Prostate Cancer|Prostate Cancer|Prostate Cancer Metastatic | Dana-Farber Cancer Institute|Puma Biotechnology Inc. | May 21 2021 | Phase 2 |
| NCT04388384 | Recruiting | Drug: Neratinib | Breast Neoplasm | Pierre Fabre Pharma GmbH|iOMEDICO AG|Pierre Fabre Pharma Austria|Pierre Fabre Pharma AG | April 20 2020 | -- |
| NCT03812393 | Recruiting | Drug: Neratinib | Triple Negative Breast Cancer|Early-stage Breast Cancer|HER2-positive Breast Cancer | West Cancer Center|Celcuity Inc.|Puma Biotechnology Inc. | June 21 2019 | Phase 2 |
| NCT03919292 | Recruiting | Drug: Neratinib|Drug: Divalproex Sodium | Solid Tumor Adult | Virginia Commonwealth University|Puma Biotechnology Inc. | May 1 2019 | Phase 1|Phase 2 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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