E-7046

Sunan Sinadari:

(S) -4- (1- (3- (difluoromethyl)) -1-methyl-5- (3- (trifluoromethyl) phenoxy) -1H-pyrazole-4-carboxamido) ethyl) benzoic acid

Lambar SMILES:

O=C(O)C1=CC=C([C@@H](NC(C2=C(OC3=CC=CC(C(F))(F)F)=C3)N(C)N=C2C (F)F=O)C)C=C1

Lambar InChi:

InChi=1S/C22H18F5N3O4/c1-11(12-6-8-13(9-7-12)21(32)33)28-19(31)16-17(18(23)24)29-30( 2)20(16)34-15-5-3-4-14(10-15)22(25,26)27/h3-11,18H,1-2H3,(H,28,31)(H, 32,33)/t11-/m0/s1

InChi Key:

MKLKAQMPKHNQPR-NSHDSACASA-N

Mabuɗin kalma:

E-7046, E7046, E 7046, 1369489-71-3

Solubility:Mai narkewa a cikin DMSO

Ajiya:0 - 4°C na gajeren lokaci (kwanaki zuwa makonni), ko -20°C na dogon lokaci (watanni).

Bayani:

A cikin ƙirar ƙwayar cuta ta CT-26, haɗin E7046/RT yana haifar da amsawar ƙwaƙwalwar ƙwayar cuta ta dabbobi 9. A cikin ƙirar 4T1, haɗin E7046 da RT kuma yana samar da ingantaccen aikin hana haɓakar ƙwayar cuta idan aka kwatanta da kowane magani kaɗai. Haɗin yana inganta rayuwa sosai ta hanyar hana ƙwayar cutar huhu ta huhu ta 4T1[1]. E7046 (150 mg/kg) yana hana haɓakar nau'ikan ƙari na syngeneic da yawa. Toshewar siginar EP4 yana haɓaka bambance-bambancen anti-tumor DC kuma yana rage jinkirin ci gaban ƙari a cikin mice. Maganin E7046 yana rage girma ko ma ƙi ciwace-ciwacen ciwace-ciwace a cikin vivo ta hanyar dogaro da ƙwayoyin myeloid da CD8C T. Bugu da ƙari kuma, haɗin gwiwar E7046 da E7777, furotin IL-2-diphtheria toxin fusion protein wanda zai fi dacewa ya kashe Tregs, synergistically yana rushe hanyoyin sadarwa na myeloid da Treg immunosuppressive, wanda ya haifar da tasiri da kuma dorewa anti-tumor amsawa a cikin linzamin kwamfuta model. .

Saukewa: EP4