Natural Supplement Raw Powder CAS 439081-18-2 BIBW 2992 for Antitumor


Quick Details:

Product Name	BIBW 2992
Synonyms	BIBW 2992; N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6- quinazolinyl]-4-(dimethylamino)-2-butenamide; Tovok; Tovok, BIBW 2992; BIBW2992 Afatinib; Afatinib (BIBW 2992); ToMtovok; (S, E)-N-(4-(3-chloro-4-fluorophenylaMino)-7
CAS register number	439081-18-2
Product Categories	API; Inhibitors
Molecular formula	C24H25ClFN5O3
Molecular weight	485.944
density	1.380
Mol File	439081-18-2. Mol
Usage	BIBW2992 (Afatinib, Tomtovok, Tovok) irreversibly inhibits EGFR/HER2 including EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively.

Product Description:

1. Afatinib (INN; trade name Gilotrif in the US and Giotrif in Europe, previously Tomtovok and Tovok[1]) is a drug approved in United States, Europe, Taiwan, Mexico, Chile and Japan as well as other countries for the first-line treatment of patients with distinct types of metastatic (EGFR mutation positive) non-small cell lung carcinoma (NSCLC), developed by Boehringer Ingelheim. It acts as an irreversible covalent inhibitor of the receptor tyrosine kinases epidermal growth factor receptor (EGFR) and erbB-2 (HER2).

2. Afatinib (BIBW 2992), a novel aniline-quinazoline derivative, irreversibly and equipotently targets the intrinsic kinase activity of all active ErbB receptor family members. Preclinical results show that afatinib is effective in lung cancer models, including those with EGF receptor (EGFR) mutations resistant to reversible first-generation EGFR inhibitors. Afatinib is being investigated in the LUX-Lung program, which will evaluate afatinib as a first-line treatment in patients with EGFR-activating mutations (LUX-Lung 2, 3 and 6) and as a second- or third-line treatment in patients that have acquired resistance to gefitinib and/or erlotinib (LUX-Lung 1, 4 and 5). LUX-Lung 1 and 2 have demonstrated, within their respective target groups, a significant increase in the disease control rate of 58 and 86%, respectively, and significant prolongation of progression-free survival.

3. Afatinib (BIBW 2992), a novel aniline-quinazoline derivative, irreversibly and equipotently targets the intrinsic kinase activity of all active ErbB receptor family members. Preclinical results show that afatinib is effective in lung cancer models, including those with EGF receptor (EGFR) mutations resistant to reversible first-generation EGFR inhibitors. Afatinib is being investigated in the LUX-Lung program, which will evaluate afatinib as a first-line treatment in patients with EGFR-activating mutations (LUX-Lung 2, 3 and 6) and as a second- or third-line treatment in patients that have acquired resistance to gefitinib and/or erlotinib (LUX-Lung 1, 4 and 5). LUX-Lung 1 and 2 have demonstrated, within their respective target groups, a significant increase in the disease control rate of 58 and 86%, respectively, and significant prolongation of progression-free survival.

Application:

Afatinib (BIBW-2992)is an irreversible, potent, orally bioavailable inhibitor of EGFR and HER2 with IC50's of 0.5 nM and 14 nM, respectively. BIBW-2992 is a second generation of tyrosine kinase inhibitor (TKI). BIBW-2992 is not only active against EGFR mutations targeted by first generation TKIs like Erlotinib or Gefitinib, but also against those not sensitive to these standard therapies. BIBW-2992 (Tovok) overcomes resistance of Tarceva in clinic. It has received regulatory approval for use as a treatment for non-small cell lung cancer, although there is emerging evidence to support its use in other cancers such as breast cancer

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