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Neratinib maleate

Catalog No. T67385 CAS 915942-22-2

Synonyms: HKI-272 maleate

Neratinib maleate (HKI-272 maleate) is an irreversible, orally active and highly selective inhibitor of HER2 and EGFR with IC50 values of 59 nM and 92 nM, respectively.Neratinib maleate has antitumor activity and can be used to treat gastrointestinal, respiratory, genitourinary, and cutaneous and musculoskeletal diseases, and can be used to study breast and prostate cancer. used in the study of breast and prostate cancer.

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Neratinib maleate, CAS 915942-22-2

Pack Size	Availability	Price/USD
25 mg	In stock	$ 40.00
50 mg	In stock	$ 57.00
100 mg	In stock	$ 82.00

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Purity: 99.64%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Neratinib maleate (HKI-272 maleate) is an irreversible, orally active and highly selective inhibitor of HER2 and EGFR with IC50 values of 59 nM and 92 nM, respectively.Neratinib maleate has antitumor activity and can be used to treat gastrointestinal, respiratory, genitourinary, and cutaneous and musculoskeletal diseases, and can be used to study breast and prostate cancer. used in the study of breast and prostate cancer.
Targets&IC50	HER2:59 nM, EGFR:92 nM
In vitro	Neratinib maleate (0.5 ng/mL–5 μg/mL; 2 days) inhibits the proliferation of cell lines that show high levels of HER-2 (3T3/neu, SK-Br-3, and BT474 (7 days)) and is much less active in cell lines that express neither HER-2 nor EGFR (3T3, MDA-MB-435, and SW620).[1] Neratinib maleate (0-2 nM; 12-16 h) arrests BT474 cell cycle at the G1-S phase.[1] Neratinib maleate results in the inhibition of MAPK and Akt phosphorylation, down-regulation of cyclin D1 levels, and induction of p27.[1]
In vivo	Neratinib maleate (HKI-272) (10, 20, 40, 60 or 80 mg/kg/day; i.g.; 42 days; Female athymic (nude) mice, tumor xenograft) reduced tumor growth in a dose-dependent manner in 3T3/neu, BT474, SK-OV-3, and A431 xenografts, but was o inactive in xenografts of MX-1 and MCF-7. Inhibited phosphorylation of HER-2 in BT474 xenografts. It shows anticancer activities against cancer cells that express high levels of HER-2 or EGFR.[1]

Synonyms	HKI-272 maleate
Molecular Weight	673.11
Formula	C34H33ClN6O7
CAS No.	915942-22-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 225.0 mg/mL (334.3 mM), Sonication is recommended.

References and Literature

1. Rabindran SK, et al. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 2004;64(11):3958-3965.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library FDA-Approved Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Anti-Cancer Compound Library

Related Products

Related compounds with same targets

PF-06459988 PP1 Sanguinarine chloride Icotinib Olmutinib PD173074 ALK/EGFR-IN-1 PD153035 hydrochloride

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Keywords

Neratinib maleate 915942-22-2 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR HER HKI 272 Maleate Neratinib Maleate HKI272 Maleate HKI-272 Maleate HKI-272 maleate inhibitor inhibit

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