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Sigma-Aldrich Neratinib
List Price $489.00 Your Price $489.00
Sigma-Aldrich Neratinib; 50 mg - SIALGSK (Additional S&H or Hazmat Fees May Apply)
NETA PART: SIALGSK-SML4231-50MG
MFG.PART: SML4231-50MG
UNSPSC: 12352200
Manufacturer: Sigma-Aldrich
Quality Level
100
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2mg/mL, clear (warmed)
storage temp.
2-8°C
SMILES string
CN(C)C/C=C/C(NC(C=C1C(NC2=CC(Cl)=C(C=C2)OCC3=NC=CC=C3)=C4C#N)=C(C=C1N=C4)OCC)=O
Biochem/physiol Actions
Irreversible pan-HER inhibitor, covalently targets EGFR/HER2/HER4, providing sustained signaling blockade and clinical benefit in HER2-positive breast cancer.
Neratinib (HKI-272), an oral, potent, irreversible pan-HER tyrosine kinase inhibitor, targets EGFR, HER2, and HER4 by covalently binding specific cysteine residues (Cys773/EGFR, Cys805/HER2) within the ATP-binding pocket. This mechanism provides prolonged target inhibition, effectively blocking HER phosphorylation (IC50 ~3-5 nM) and downstream MAPK/Akt signaling (IC50 ~2 nM). Consequently, it reduces cyclin D1/Rb phosphorylation (IC50 ~9 nM) and induces G1-S arrest and apoptosis in sensitive cell lines (e.g., BT474, SKBr3, A431) at low nM concentrations, underpinning its use against HER2-driven cancers.
Neratinib (HKI-272), an oral, potent, irreversible pan-HER tyrosine kinase inhibitor, targets EGFR, HER2, and HER4 by covalently binding specific cysteine residues (Cys773/EGFR, Cys805/HER2) within the ATP-binding pocket. This mechanism provides prolonged target inhibition, effectively blocking HER phosphorylation (IC50 ~3-5 nM) and downstream MAPK/Akt signaling (IC50 ~2 nM). Consequently, it reduces cyclin D1/Rb phosphorylation (IC50 ~9 nM) and induces G1-S arrest and apoptosis in sensitive cell lines (e.g., BT474, SKBr3, A431) at low nM concentrations, underpinning its use against HER2-driven cancers.
| SKU | SIALGSK-SML4231-50MG |
|---|---|
| Supplier Part Number | SML4231-50MG |
| UM | EA |
| UNSPSC | 12352200 |
| Manufacturer | Sigma-Aldrich |
| ProductLine | SIALGSK |
| Qty | 1 |
| MinOrderQty | 1 |
| Weight | 7.000000 |
| Lead Time | 9 |
| CAS Number | 698387-09-6 |
| Energy Star | No |
| Green | No |
| Controlled | N |