Neratinib Maleate
- CAS NO.:915942-22-2
- Empirical Formula: C34H33ClN6O7
- Molecular Weight: 673.12
- MDL number: MFCD30607264
- EINECS: 620-527-5
- Update Date: 2024-11-12 15:22:14
What is Neratinib Maleate?
Description
Neratinib (HKI-272) is a pan-HER inhibitor, this irreversible tyrosine kinase inhibitor binds and inhibits the tyrosine kinase activity of epidermal growth factor receptors, EGFR (or HER1), HER2 and HER4, which leads to reduced phosphorylation and activation of downstream signaling pathways.
The Uses of Neratinib Maleate
A drug used alone or with capecitabine to treat adults with certain types of HER2-positive breast cancer that have already been treated. It is also being studied in the treatment of other types of cancer. Neratinib maleate blocks certain proteins, which may help keep cancer cells from growing and may kill them. It is a type of tyrosine kinase inhibitor.
The Uses of Neratinib Maleate
Neratinib Maleate is a codrug; used in preparation of heterobifunctional PROTAC compounds as degraders of estrogen receptor.
Biological Activity
Neratinib is a modified form of the discontinued compound pelitinib, and was originally being develoAdditionally, phase II development of oral neratinib as a neoadjuvant therapy for breast cancer, as a second-line therapy for non-small cell lung cancer, and for other solid tumours is also in progress in numerous countries worldwide. ped by Wyeth (later Pfizer). Oral neratinib is awaiting approval as an extended adjuvant therapy for breast cancer in the EU and in the US. Blocking HER2 function by a small molecule kinase inhibitor, such as neratinib, represents an attractive alternate strategy for the growth inhibition of HER2-positive tumours.
Mechanism of action
Neratinib Maleate is the maleate salt form of neratinib, an orally available, quinazoline-based, irreversible inhibitor of both the receptor tyrosine kinases (RTKs) human epidermal growth factor receptor 2 (HER2; ERBB2) and human epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon administration, neratinib targets and covalently binds to the cysteine residue in the ATP-binding pockets of both HER2 and EGFR. This inhibits their activity and results in the inhibition of downstream signal transduction events, induces cell cycle arrest, apoptosis and ultimately decreases cellular proliferation in HER2- and EGFR-expressing tumor cells. EGFR and HER2, RTKs that are mutated or overactivated in many tumor cell types, play key roles in tumor cell proliferation and tumor vascularization.
Properties of Neratinib Maleate
storage temp. | Inert atmosphere,Room Temperature |
form | Solid |
color | White to off-white |
Safety information for Neratinib Maleate
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Neratinib Maleate
New Products
(R)-3-Aminobutanenitrile Hydrochloride 4-Aminotetrahydropyran-4-carbonitrile Hydrochloride 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine SODIUM AAS SOLUTION ZINC AAS SOLUTION BUFFER SOLUTION PH 10.0(BORATE) GOOCH CRUCIBLE SINTERED AQUANIL 5 BERYLLIUM AAS SOLUTION SODIUM VALPROATE Diclofenac Sodium Methylcobalamin (vitamin B12) VILDAGLIPTIN ACICLOVIR AMOXICILLIN (AMOXYCILLIN) TRIHYDRATE Desloratidine Related compound B Folic Acid Impurity G Glycopyrronium Bromide EP Impurity I Eltrombopag N-Oxide Impurity Di-Nitroso Acyclovir Impurity K DLRD N-OxideRelated products of tetrahydrofuran
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