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Chemodex
Neratinib
108
CHF
CHF 108.00
In stock
CDX-N0326-M05050 mgCHF 108.00
CDX-N0326-M100100 mgCHF 162.00
CDX-N0326-M250250 mgCHF 326.00
| Product Details | |
|---|---|
| Synonyms | HKI-272 |
| Product Type | Chemical |
| Properties | |
| Formula | C30H29ClN6O3 |
| MW | 557 |
| CAS | 698387-09-6 |
| Purity Chemicals | ≥98% |
| Appearance | Off-white powder. |
| Solubility | Soluble in DMSO (2mg/ml). Insoluble in water. |
| Identity | Determined by 1H-NMR. |
| Declaration | Manufactured by Chemodex. |
| Other Product Data |
Click here for Original Manufacturer Product Datasheet |
| InChi Key | JWNPDZNEKVCWMY-VQHVLOKHSA-N |
| Smiles | CCOC1=C(NC(/C=C/CN(C)C)=O)C=C(C(NC2=CC(Cl)=C(OCC3=NC=CC=C3)C=C2)=C(C#N)C=N4)C4=C1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Protect from light and moisture. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS | Inquire |
| Product Specification Sheet | |
| Datasheet |
 Download PDF |
Description
Neratinib is a cell-permable, irreversible, selective inhibitor of the HER2 kinase (IC50=59nM) and EGFR (IC50=92nM) by preventing phosphorylation of these proteins by their respective kinases. It also potently inhibits several mutants of HER2 and shows 10-fold or greater selectivity over a wide variety of other kinases. As an irreversible inhibitor, neratinib may circumvent acquired resistance developed against reversible inhibitors, including gefitinib. Neratinib displays activity against a variety of cancer cell lines, including A431, 3T3, and MDA-MB-435. Neratinib has been evaluated in clinical trials against cancers characterized by HER2 overexpression or HER2 activating mutations.
Product References
(1) S.K. Rabindran, et al.; Cancer Res. 64, 3958 (2004) | (2) E.L. Kwak, et al.; PNAS 102, 7665 (2005) | (3) H. Ji, et al.; PNAS 103, 7817 (2006) | (4) P. Bose & H. Ozer; Expert. Opin. Investig. Drugs 18, 1735 (2009) (Review) | (5) M.I. Davis, et al.; Nat. Biotechnol. 29, 1046 (2011) | (6) S.M. Kavuri, et al.; Cancer Discov. 5, 832 (2015) | (7) M. Segovia-Mendoza, et al.; Am. J. Cancer Res. 5, 2531 (2015) | (8) S.R. Tiwari, et al.; Clin. Breast Cancer 16, 344 (2016) (Review)