Neratinib

5 mg

Cat. No.: 50-P44

$149.00

Neratinib, also known as HKI-272, is a second-generation inhibitor of the ErbB family of receptor kinases. Neratinib is an irreversible inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER-2) tyrosine kinases by targeting a cysteine residue in the ATP-binding site of the receptor.  Neratinib has been shown to inhibit the proliferation of HER-2 overexpressing human breast cancer cell lines and EGFR-dependent cells in vitro. In vivo, Neratinib has been shown to be active against HER-2- and EGFR-dependent tumor xenograft models .

 

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TECHNICAL INFORMATION

Other Names: HKI-272

Chemical Formula: C30H29ClN6O3

CAS Number: 698387-09-6

Molecular Weight: 557.04

Purity:  >98%

Appearance:  a crystalline solid  

Solubility: DMSO

 

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light. Following reconstitution, store  aliquots at -20°C. 

Stability: Stock solutions stable at -20°C for up to 2 years.

Shipping Conditions: Shipped at room temperature.

 

PRODUCT USE

Soluble in DMSO at 2 mg/ml. If precipitate is observed,  vortex for 5 minutes. For most cells, the maximum tolerance to DMSO is less than 0.5%. 

References

Sequist LV. (2007) Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer. Oncologist. 12(3):325-30.

Rabindran et al. (2004) Antitumor activity of HKI-272 | an orally active | irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 64(11):3958-65.

Li et al. (2007) Bronchial and peripheral murine lung carcinomas induced by T790M-L858R mutant EGFR respond to HKI-272 and rapamycin combination therapy. Cancer Cell. 12(1):81-93.

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