Neratinib

For research use only. Not for therapeutic Use.

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Neratinib(CAT: I004621) is an orally available small-molecule inhibitor that targets several tyrosine kinases, including HER1 (EGFR), HER2 (ErbB2), and HER4 (ErbB4). It is used for the treatment of certain types of breast cancer, particularly HER2-positive breast cancer, which is characterized by an overexpression of HER2 receptors. Neratinib works by irreversibly binding to the tyrosine kinase domains of these receptors, thereby inhibiting their signaling pathways involved in cell growth and proliferation. This inhibition helps to suppress the growth and spread of cancer cells.


Catalog Number I004621
CAS Number 698387-09-6
Synonyms

HKI-272

Molecular Formula C₃₀H₂₉ClN₆O₃
Purity ≥95%
Target EGFR
Solubility DMSO:< 5.6 mg/mL
Storage Store at -20°C
IC50 59 nM/92 nM (HER2/EGFR)
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
SMILES CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)C=CCN(C)C
Reference

1: Chow LW, Xu B, Gupta S, Freyman A, Zhao Y, Abbas R, Vo Van ML, Bondarenko I.
Combination neratinib (HKI-272) and paclitaxel therapy in patients with
HER2-positive metastatic breast cancer. Br J Cancer. 2013 May 28;108(10):1985-93.
doi: 10.1038/bjc.2013.178. Epub 2013 Apr 30. PubMed PMID: 23632474; PubMed
Central PMCID: PMC3670493. <br />
2: Zhao XQ, Xie JD, Chen XG, Sim HM, Zhang X, Liang YJ, Singh S, Talele TT, Sun
Y, Ambudkar SV, Chen ZS, Fu LW. Neratinib reverses ATP-binding cassette
B1-mediated chemotherapeutic drug resistance in vitro, in vivo, and ex vivo. Mol
Pharmacol. 2012 Jul;82(1):47-58. doi: 10.1124/mol.111.076299. Epub 2012 Apr 4.
PubMed PMID: 22491935; PubMed Central PMCID: PMC3382829. <br />
3: López-Tarruella S, Jerez Y, Márquez-Rodas I, Martín M. Neratinib (HKI-272) in
the treatment of breast cancer. Future Oncol. 2012 Jun;8(6):671-81. doi:
10.2217/fon.12.66. Review. PubMed PMID: 22764764. <br />
4: Burstein HJ, Sun Y, Dirix LY, Jiang Z, Paridaens R, Tan AR, Awada A, Ranade A,
Jiao S, Schwartz G, Abbas R, Powell C, Turnbull K, Vermette J, Zacharchuk C,
Badwe R. Neratinib, an irreversible ErbB receptor tyrosine kinase inhibitor, in
patients with advanced ErbB2-positive breast cancer. J Clin Oncol. 2010 Mar
10;28(8):1301-7. doi: 10.1200/JCO.2009.25.8707. Epub 2010 Feb 8. PubMed PMID:
20142587. <br />
5: Wong KK, Fracasso PM, Bukowski RM, Lynch TJ, Munster PN, Shapiro GI, J&#228;nne PA,
Eder JP, Naughton MJ, Ellis MJ, Jones SF, Mekhail T, Zacharchuk C, Vermette J,
Abbas R, Quinn S, Powell C, Burris HA. A phase I study with neratinib (HKI-272),
an irreversible pan ErbB receptor tyrosine kinase inhibitor, in patients with
solid tumors. Clin Cancer Res. 2009 Apr 1;15(7):2552-8. doi:
10.1158/1078-0432.CCR-08-1978. Epub 2009 Mar 24. PubMed PMID: 19318484.

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