Neratinib | HER2/ErbB2 and EGFR kinase inhibitor
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 20 mg | $50.00 | ||
| 100 mg | $120.00 |
Neratinib (698387-09-6) is a potent, irreversible inhibitor of HER2/ErbB2 receptor tyrosine kinase and EGFR kinase (IC50’s= 59 nM and 92 nM, respectively). It suppresses receptor autophosphorylation and proliferation, blocks cell-cycle progression and inhibits HER2 signaling in of EGFR-dependent cancer cells and tumor xenograft models.1 Neratinib inhibits proliferation of gefitinib-resistant non-small cell lung cancer cells expressing mutant EGFR.2 Synergizes with dasatinib in HER2-positive cancer cells and xenografts.3 It’s been shown to also inhibit MST1 (IC50 = 37.7 nM).4
References/Citations:
- Rabindran et al. (2004), Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase; Cancer Res. 64 3958
- Kwak et al. (2005), Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib; Proc. Natl. Acad. Sci. USA 102 7665
- Conlon et al. (2024), Neratinib plus Dasatinib is highly synergistic in HER2-positive breast cancer in vitro and in vivo; Trans. Oncol. 49 102073
- Yun et al. (2008), The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP; Proc. Natl. Acad. Sci. USA 105 20770
C30H29ClN6O3
>98% HPLC
NMR: (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
Neratinib (698387-09-6) is a potent, irreversible inhibitor of HER2/ErbB2 receptor tyrosine kinase and EGFR kinase (IC50’s= 59 nM and 92 nM, respectively). It suppresses receptor autophosphorylation and proliferation, blocks cell-cycle progression and inhibits HER2 signaling in of EGFR-dependent cancer cells and tumor xenograft models.1 Neratinib inhibits proliferation of gefitinib-resistant non-small cell lung cancer cells expressing mutant EGFR.2 Synergizes with dasatinib in HER2-positive cancer cells and xenografts.3 It’s been shown to also inhibit MST1 (IC50 = 37.7 nM).4
References/Citations:
- Rabindran et al. (2004), Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase; Cancer Res. 64 3958
- Kwak et al. (2005), Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib; Proc. Natl. Acad. Sci. USA 102 7665
- Conlon et al. (2024), Neratinib plus Dasatinib is highly synergistic in HER2-positive breast cancer in vitro and in vivo; Trans. Oncol. 49 102073
- Yun et al. (2008), The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP; Proc. Natl. Acad. Sci. USA 105 20770
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