Neratinib CAS: 698387-09-6
MF: C30H29ClN6O3
MW: 557.04
A potent and selective inhibitor of EGFR and HER2.

Neratinib (CAS 698387-09-6)

Neratinib | CAS 698387-09-6 is rated 5.0 out of 5 by 1.
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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 (including water content).

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.


References

1. Rabindran SK, et al. Cancer Res, 2004, 64(11), 3958-3965.

Appearance :
Crystalline granules or crystalline powder
Physical State :
Solid
Solubility :
Soluble in DMSO (2 mg/ml at 25° C), water (<1 mg/ml at 25° C), and ethanol (<1 mg/ml at 25° C).
Storage :
Store at -20° C
Melting Point :
139-158° C
Boiling Point :
~757.0° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.67 (Predicted)
IC50 :
HER2: IC50 = 59 nM; Proliferation of EGFR-dependent A431 cells : IC50 = 81 nM; EGFR: IC50 = 92 nM; Tyrosine kinases KDR: IC50 = 0.8 µM; Src: IC50 = 1.4 µM
pK Values :
pKa: 12.37 (Predicted), pKb: 8.01 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
9915743
MDL Number :
MFCD09752958
SMILES :
CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)/C=C/CN(C)C

Download SDS (MSDS)

Certificate of Analysis

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Neratinib (CAS 698387-09-6)  Product Citations

See how others have used Neratinib (CAS 698387-09-6). Click on the entry to view the PubMed entry .

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PMID: # 30462579  Paatero, I.|Veikkolainen, V.|Mäenpää, M.|Schmelzer, E.|Belting, HG.|Pelliniemi, LJ.|Elenius, K.| et al. 2019. Mol. Biol. Cell. 30: 209-218.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Schwab et al Schwab et al. (PubMed ID 26260909) found that Neratinib inhibited carcinosarcoma proliferation via HER2/neu inhibition. -SCBT Publication Review
Date published: 2015-03-23
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