Nazartinib; EGF816; NVS-816

Orukọ Kemikali:

(R, E) -N- (7-chloro-1- (1-- (4--dimethylamino)sugbon-2-enoyl)azepan-3-yl) -1H-benzo [d] imidazol-2-yl)- 2-methylisonicotinamide

KỌỌDỌ SMILES:

O=C(NC1=NC2=CC=CC(Cl)=C2N1[C@H]3CN(C(/C=C/CN(C)C)=O)CCCC3)C4=CC=NC(C)= C4

Koodu InChi:

InChi=1S/C26H31ClN6O2/c1-18-16-19(12-13-28-18)25(35)30-26-29-22-10-6-9-21(27)24(22)33( 26)20-8-4-5-15-32 (17-20)23 (34)11-7-14-31 (2)3/h6-7,9-13,16,20H,4-5, 8,14-15,17H2,1-3H3,(H,29,30,35)/b11-7+/t20-/m1/s1

Bọtini InChi:

IOMMMLWIABWRKL-WUTDNEBXSA-N

Koko-ọrọ:

Nazartinib ,EGF816, EGF-816, EGF 816, NVS-816, 1508250-71-2

Solubility:Tiotuka ni DMSO

Ibi ipamọ:0 - 4°C fun igba kukuru (ọjọ si awọn ọsẹ), tabi -20°C fun igba pipẹ (osu)

Apejuwe:

Nazartinib, ti a tun mọ ni EGF816 ati NVS-816, jẹ ẹnu-ọrọ ti o wa, ti ko ni iyipada, iran-kẹta, oludena idagba ifosiwewe idagba mutant-yan, pẹlu iṣẹ-ṣiṣe antineoplastic ti o pọju. EGF816 covalently sopọ si ati ṣe idiwọ iṣẹ ṣiṣe ti awọn fọọmu mutant ti EGFR, pẹlu ẹda T790M EGFR, nitorinaa idilọwọ ifihan agbara-alaja EGFR. Eyi le fa iku sẹẹli jẹ ki o dẹkun idagbasoke tumo ni EGFR-overexpressing tumo awọn sẹẹli. EGF816 ni pataki ṣe idiwọ awọn fọọmu iyipada ti EGFR pẹlu T790M, iyipada resistance ti o gba ni ẹẹkeji, ati pe o le ni awọn anfani itọju ailera ninu awọn èèmọ pẹlu T790M resistance ti o ni agbedemeji nigba akawe si awọn inhibitors EGFR tyrosine kinase miiran.

afojusun: EGFR