Date published: 2026-4-24

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Neratinib (CAS 698387-09-6)

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Alternate Names:
HKI-272
Application:
Neratinib is a potent and selective inhibitor of EGFR and HER2
CAS Number:
698387-09-6
Purity:
≥99%
Molecular Weight:
557.04
Molecular Formula:
C30H29ClN6O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Neratinib is a potent and selective inhibitor of EGFR and Neu(HER2) (IC50 = 92 nM and 59 nM, respectively) by preventing phosphorylation of these proteins by their respective kinases. Neratinib displays activity against a variety of cancer cell lines, including A431, 3T3, and MDA-MB-435. Neratinib is an inhibitor of c-Src and Flk-1.


Neratinib (CAS 698387-09-6) References

  1. Neratinib (HKI-272) in the treatment of breast cancer.  |  López-Tarruella, S., et al. 2012. Future Oncol. 8: 671-81. PMID: 22764764
  2. Profile of neratinib and its potential in the treatment of breast cancer.  |  Feldinger, K. and Kong, A. 2015. Breast Cancer (Dove Med Press). 7: 147-62. PMID: 26089701
  3. Neratinib, A Novel HER2-Targeted Tyrosine Kinase Inhibitor.  |  Tiwari, SR., et al. 2016. Clin Breast Cancer. 16: 344-348. PMID: 27405796
  4. Neratinib: First Global Approval.  |  Deeks, ED. 2017. Drugs. 77: 1695-1704. PMID: 28884417
  5. Neratinib for the Treatment of Early-Stage HER2-Positive Breast Cancer.  |  Miles, J. and White, Y. 2018. J Adv Pract Oncol. 9: 750-754. PMID: 31249722
  6. Mechanism, safety and efficacy of three tyrosine kinase inhibitors lapatinib, neratinib and pyrotinib in HER2-positive breast cancer.  |  Xuhong, JC., et al. 2019. Am J Cancer Res. 9: 2103-2119. PMID: 31720077
  7. Neratinib: the emergence of a new player in the management of HER2+ breast cancer brain metastasis.  |  Nasrazadani, A. and Brufsky, A. 2020. Future Oncol. 16: 247-254. PMID: 32057254
  8. Neratinib plus capecitabine for the treatment of advanced HER2-positive breast cancer.  |  Oliveira, M., et al. 2020. Expert Rev Anticancer Ther. 20: 731-741. PMID: 32862744
  9. Combining Neratinib with CDK4/6, mTOR, and MEK Inhibitors in Models of HER2-positive Cancer.  |  Zhao, M., et al. 2021. Clin Cancer Res. 27: 1681-1694. PMID: 33414137
  10. Osimertinib-resistant NSCLC cells activate ERBB2 and YAP/TAZ and are killed by neratinib.  |  Dent, P., et al. 2021. Biochem Pharmacol. 190: 114642. PMID: 34077739
  11. The Clinical Efficacy and Safety of Neratinib in Combination with Capecitabine for the Treatment of Adult Patients with Advanced or Metastatic HER2-Positive Breast Cancer.  |  Chilà, G., et al. 2021. Drug Des Devel Ther. 15: 2711-2720. PMID: 34188449
  12. Neratinib causes non-recoverable gut injury and reduces intestinal cytochrome P450 3A enzyme in mice.  |  Tao, G., et al. 2022. Toxicol Res (Camb). 11: 184-194. PMID: 35237423
  13. Mechanisms of neratinib resistance in HER2-mutant metastatic breast cancer.  |  Eli, LD. and Kavuri, SM. 2022. Cancer Drug Resist. 5: 873-881. PMID: 36627899

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Neratinib, 5 mg

sc-364549
5 mg
$92.00

Neratinib, 25 mg

sc-364549A
25 mg
$214.00

Neratinib, 100 mg

sc-364549B
100 mg
$383.00

Neratinib, 500 mg

sc-364549C
500 mg
$755.00

Neratinib, 1 g

sc-364549D
1 g
$1250.00