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Neratinib
- HKI 272
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C30H29ClN6O3
- MW: 557.04
Description
Neratinib (HKI-272) is an irreversible tyrosine kinase inhibitor targeting HER2/ErbB2 and EGFR/ErbB1 signaling.
ErbB receptor signaling drives proliferation, survival and therapeutic resistance in multiple tumor types. Neratinib is useful for studying covalent HER-family kinase inhibition, HER2-dependent cancer biology and EGFR/HER2 pathway blockade in cellular models.
Key Features
- Irreversible HER2 and EGFR tyrosine kinase inhibitor
- Blocks oncogenic ErbB receptor signaling
- Relevant to HER2-driven breast cancer research
- Useful for studies of covalent kinase inhibition and resistance
Applications
- HER2/EGFR signaling research
- Breast and epithelial cancer models
- ErbB kinase inhibitor profiling
- Drug-resistance and combination studies
More Information
| Parent CAS No. | 698387-09-6 |
|---|---|
| Chemical Name | (E)-4-Dimethylamino-but-2-enoic acid {4-[3-chloro-4-(pyridin-2-ylmethoxy)-phenylamino]-3-cyano-7-ethoxy-quinolin-6-yl}-amide |
| SMILES | C1(OCC)C=C2N=CC(C#N)=C(NC3C=CC(OCC4C=CC=CN=4)=C(Cl)C=3)C2=CC=1NC(=O)/C=C/CN(C)C |
| MFCD | MFCD09752958 |
| InChi | InChI=1S/C30H29ClN6O3/c1-4-39-28-16-25-23(15-26(28)36-29(38)9-7-13-37(2)3)30(20(17-32)18-34-25)35-21-10-11-27(24(31)14-21)40-19-22-8-5-6-12-33-22/h5-12,14-16,18H,4,13,19H2,1-3H3,(H,34,35)(H,36,38)/b9-7+ |
| InChiKey | JWNPDZNEKVCWMY-VQHVLOKHSA-N |
| CID | 9915743 |
| Short Description | EGFR/HER2 inhibitor |
References
- SK Rabindran et al. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 2004, 64(11), 3958–65.
- Y Minami et al. The major lung cancer-derived mutants of ERBB2 are oncogenic and are associated with sensitivity to the irreversible EGFR/ERBB2 inhibitor HKI-272. Oncogene 2007, 26(34), 5023–7.
- A Ocaña and E Amir. Irreversible pan-ErbB tyrosine kinase inhibitors and breast cancer: current status and future directions. Cancer Treat Rev. 2009, 5(8), 685-691.
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