Afatinib (BIBW 2992) Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

In July 2013, the US FDA approved afatinib (also referred to as BIBW- 2992), for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) and with tumors that have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution. Afatinib functions as an irreversible inhibitor by covalently binding directly to the ATP-binding site in the kinase domains of both EGFR(Cys 773) andHER2 (Cys 805;HER-2 is the preferred dimerization partner of EGFR) resulting in downregulation of EGFR signaling. Afatinib is a potent inhibitor of wild-type and mutant forms (L858R) of EGFR (IC_50s of 0.5 and 0.4 nM, respectively), and HER2 (IC₅₀=14 nM), but about 100-fold more active against the gefitinib resistant L858R– T790M EGFR double mutant, with an IC₅₀ of 10 nM. Consistent with its in vitro activity, afatinib induces tumor regression in xenograft and transgenic lung cancer models, with superior activity over erlotinib. A synthetic route to afatinib that employs the displacement of a phenylsulfonyl group to install the (S)-3-hydoxytetrahydrofuran ring and a modified Horner–Wadsworth–Emmons reaction with {[4-(3-chloro-4- phenylamino)-7-((S)-tetrahydrofuran-3-yloxy)-quinazolin-6-ylcarbamoyl]- methyl}-phosphonate and dimethylaminoacetaldehyde-hydrogen sulfite adduct to install the eneamide moiety, has been reported.

Verwenden

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.

Afatinib (BIBW 2992) Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Afatinib (BIBW 2992) Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Hebei Weibang Biotechnology Co., Ltd	+8615531157085	abby@weibangbio.com	China	8810	58
Hebei Mojin Biotechnology Co., Ltd	+86 13288715578 +8613288715578	sales@hbmojin.com	China	12835	58
Hebei Yanxi Chemical Co., Ltd.	+8617531190177	peter@yan-xi.com	China	5857	58
shandong perfect biotechnology co.ltd	+86-53169958659 +86-13153181156	sales@sdperfect.com	China	294	58
Henan Fengda Chemical Co., Ltd	+86-371-86557731 +86-13613820652	info@fdachem.com	China	20284	58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.	+86-18600796368 +86-18600796368	sales@sjar-tech.com	China	456	58
Hebei Zhuanglai Chemical Trading Co Ltd	+86-16264648883 +86-16264648883	niki@zlchemi.com	China	2691	58
Capot Chemical Co.,Ltd.	+86-（0）57185586718 +86-13336195806	sales@capot.com	China	29791	60
Beijing Cooperate Pharmaceutical Co.,Ltd	010-60279497	sales01@cooperate-pharm.com	CHINA	1803	55
Shanghai Bojing Chemical Co.,Ltd.	+86-86-02137122233 +8613795318958	bj1@bj-chem.com	China	299	55

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• Tovok
• Afatinb
• (S)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dim
• Tovok, BIBW 2992
• BIBW 2992;TOVOK
• BIBW2992 Afatinib
• Afatinib (BIBW 2992)
• ToMtovok
• (S,E)-N-(4-(3-chloro-4-fluorophenylaMino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl)-4-(diMethylaMino)but-2-enaMide
• (E)-N-(7-((S)-tetrahydrofuran-3-yloxy)-4-(3-chloro-4-fluorophenylaMino)quinazolin-6-yl)-4-(diMethylaMino)but-2-enaMide
• (S)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dimeth
• (S,E)-N-(4-(3-chloro-4-fluorophenylaMino)-7-(tetrahydrofuran-2-yloxy)quinazolin-6-yl)-4-(diMethylaMino)but-2-enaMide
• (S)-N-(4-((3-Chloro-4-fluorophenyl)aMino)-7-((tetrahydrofuran- 3-yl)oxy)quinazolin-6-yl)-4-(diMethylaMino)but-2-enaMide
• BIBW 2992 N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide
• Afatinib, Free Base
• Tofacitinib and its interMediate
• Afatinib, >=99%
• Afatinib (BIBW 2992)r
• Afatinib (BIBW 2992) powder
• (E/Z)-Afatinib
• Afatinib(cis-trans isomerismtautomers)
• Afatinib(W.S)
• AFATINIB; BIBW2992;BIBW-2292
• BIBW-2292
• CS-95
• TOVOK (BIBW-2992, Afatinib)
• 2992
• (S)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[(3-tetrahydrofuranyl)oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide
• [14C]Afatinib
• [14C] (S)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dim
• 2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-
• Cancer Treatment Afatinib CAS
• Medicine Grade Afatinib
• Afatinib (BIBW 2992) USP/EP/BP
• BIBW 2992
• N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide
• (E)-N-[4-(3-chloro-4-fluoroanilino)-7-[(3S)-oxolan-3-yl]oxyquinazolin-6-yl]-4-(dimethylamino)but-2-enamide
• Alfatinib
• The method for
• Afatinib Base
• Offer 439081-18-2 Afatinib (BIBW 2992)
• Afatinib 99%
• N-4-(3-Chloro-4-fluorophenyl)amino-7-(3S)-tetrahydro-furan-3-yloxy-6-quinazolinyl-4-(dimethylamino)but-2-enamide
• (S)-Afatinib
• N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[(3S)-oxolan-3-yloxy]quinazolin-6-yl}-4-(dimethylamino)but-2-enamide
• 439081-18-2
• 439081-18-0
• API
• Inhibitors