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trans-4-Dimethylaminocrotonic Acid Hydrochloride CAS 848133-35-7 Purity >98.0% (HPLC) Afatinib Dimaleate Intermediate

Manufacturer Supply, High Purity, Commercial Production
Chemical Name trans-4-Dimethylaminocrotonic Acid Hydrochloride
Synonyms trans 4-Dimethylaminocrotonic Acid HCl; (E)-4-(Dimethylamino)-2-Butenoic Acid Hydrochloride; (E)-4-Dimethylaminocrotonic Acid Hydrochloride; (2E)-4-(Dimethylamino)but-2-Enoic Acid Hydrochloride
CAS Number 848133-35-7
CAT Number RF-PI2029
Stock Status In Stock, Production Capacity 200MT/Year
Molecular Formula C6H12ClNO2
Molecular Weight 165.62
Sensitivity Moisture Sensitive
Melting Point 160.0 to 164.0℃
Solubility DMSO (Slightly), Methanol (Slightly), Water (Slightly)
Brand Ruifu Chemical
Item Specifications
Appearance White to Almost White Powder
Purity / Analysis Method >99.0% (HPLC)
Purity / Analysis Method >99.0% (Neutralization Titration)
Moisture (K.F) <0.50%
Residue on Ignition <0.20%
Single Impurity <0.50%
Total Impurities <1.00%
Heavy Metals (as Pb) <20ppm
Infrared Spectrum Conforms to Structure
Proton NMR Spectrum Proton NMR Spectrum
Test Standard Enterprise Standard
Usage Intermediate of Afatinib, Afatinib Dimaleate
Package: Bottle, Aluminium foil bag, 25kg/Cardboard Drum, or according to customer's requirement Storage Condition: Store in sealed containers at cool and dry place; Protect from light and moisture trans-4-Dimethylaminocrotonic Acid Hydrochloride (CAS: 848133-35-7) is a reagent used in the preparation of tyrosine kinase inhibiting antitumor agents. trans-4-Dimethylaminocrotonic Acid Hydrochloride can be used as an intermediate of Afatinib (CAS: 439081-18-2), Afatinib Dimaleate (CAS: 850140-73-7), Neratinib (CAS: 698387-09-6). Afatinib is a drug approved for the treatment non-small cell lung carcinoma (NSCLC), developed by Boehringer Ingelheim. It acts as a angiokinase inhibitor. Like Lapatinib and Neratinib, Afatinib is a tyrosine kinase inhibitor (TKI) that also irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. Afatinib is not only active against EGFR mutations targeted by first generation TKIs likeerlotinib or gefitinib, but also against those not sensitive to these standard therapies. Because of its additional activity against Her2, it is being investigated for breast cancer as well as other EGFR and Her2 driven cancers. Neratinib developed by US Wyeth company is an irreversible epidermal growth factor receptor(EGFR) inhibitor. It is a multiple target point of small molecule tyrosine kinase inhibitors to HER 2 and HER1 after Lapatinib, and is an irreversible ErbB receptor tyrosine kinase inhibitor. Neratinib could selectively inhibit HER-1 and HER-2 of EGFR family(IC50 was 92 nmol/L and 59 nmol/L, respectively). Clinical research showed that Neratinib exerted significant therapeutic effect on non-small cell lung cancer, colon cancer, and breast cancer. The phaseⅡclinical trial indicated that Neratinib showed good efficacy and tolerance to HER-2 positive patients with advanced breast cancer who had been received or not Trastuzumab treatment. The phase Ⅲ breast cancer clinical trial was complete in September 2014.