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EGFR protein kinase inhibitor Neratinib, 5 mg  

EGFR protein kinase inhibitor Neratinib, 5 mg

(E)-4-Dimethylamino-but-2-enoic acid {4-[3-chloro-4-(pyridin-2-ylmethoxy)-phenylamino]-3-cyano-7-ethoxy-quinolin-6-yl}-amide

Synonyms: HKI 272
Neratinib is an irreversible tyrosine kinase inhibitor with activity against HER2 and EGFR kinases.

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PKI-NRTB-005

Availability: within 3 days

136,50 €

Background: Neratinib - HKI 272 is an irreversible tyrosine kinase inhibitor with activity against HER2 and EGFR kinases with IC50 of 59 nM and 92 nM; no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. HKI 272 is a therapeutic agent under investigation for the treatment breast cancer and other solid tumors.

Chemical formula: C30H29ClN6O3
Molecular weight: 557.04 g/mol
Purity: 98%
Appearance: Yellow solid
Solubility: Soluble in 0.1N HCl(aq) and DMSO
CAS Number: 698387-09-6

Manufacturer:  Axon Medchem BV

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers. 

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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