Neratinib, Free Base

Neratinib, Free Base
Item number Size Datasheet Manual SDS Delivery time Quantity Price
LC-N-6404_5mg 5 mg - -

3 - 15 business days*

62.00€
LC-N-6404_10mg 10 mg - -

3 - 15 business days*

74.00€
LC-N-6404_25mg 25 mg - -

3 - 15 business days*

93.00€
LC-N-6404_50mg 50 mg - -

3 - 15 business days*

109.00€
LC-N-6404_100mg 100 mg - -

3 - 15 business days*

156.00€
LC-N-6404_200mg 200 mg - -

3 - 15 business days*

259.00€
LC-N-6404_500mg 500 mg - -

3 - 15 business days*

385.00€
LC-N-6404_1g 1 g - -

3 - 15 business days*

647.00€
LC-N-6404_2g 2 g -

3 - 15 business days*

1,010.00€
 
Solubility: Soluble in DMSO at 2 mg/mL with warming, very poorly soluble in ethanol, very poorly... more
Product information "Neratinib, Free Base"
Solubility: Soluble in DMSO at 2 mg/mL with warming, very poorly soluble in ethanol, very poorly soluble in water, maximum solubility in plain water is estimated to be about 5-20 µM, buffers, serum, or other additives may increase or decrease the aqueous solubility. Neratinib, also known as HKI-272, is considered to be a second-generation inhibitor of the ErbB family of receptor kinases. Sequist, L.V., et al. 'Second-Generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non-Small Cell Lung Cancer.' Oncologist 12: 325-330 (2007). 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. Rabindran, S.K., et al. 'Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase.' Cancer Res. 64: 3958-3965 (2004). Neratinib inhibits the proliferation of HER-2 overexpressing human breast cancer cell lines and EGFR-dependent cells in vitro. In vivo, neratinib is active against HER-2- and EGFR-dependent tumor xenograft models. Rabindran, S.K., et al. 'Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase.' Cancer Res. 64: 3958-3965 (2004). Acquired resistance of non-small cell lung cancers to gefitinib because of a T790M mutation in the EGFR kinase domain is circumvented by neratinib. Kwak, E.L., et al. 'Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib.' Proc. Natl. Acad. Sci. USA 102: 7665-7670 (2005). Neratinib is active against HER-2-positive breast cancer in patients. Wong, K.K., et al. 'HKI-272, an irreversible pan erbB receptor tyrosine kinase inhibitor: Preliminary phase 1 results in patients with solid tumors.' J. Clin. Oncol. 24: 3018 (2006).
Keywords: HKI-272
Supplier: LC Laboratories
Supplier-Nr: N-6404

Properties

Application: EGFR/ ERBB2 inhibitor
MW: 557,04 D
Formula: C30H29ClN6O3
Purity: >99%

Database Information

CAS : 698387-09-6| Find alternatives
KEGG ID : K04361 | Find alternatives

Handling & Safety

Storage: -20°C
Shipping: +20°C (International: °C)
Signal Word: Warning
GHS Hazard Pictograms:
H Phrases: H335, H361, H303, H313, H333
P Phrases: P261, P264, P280, P314, P308+P311, P501
Caution
Our products are for laboratory research use only: Not for administration to humans!
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