E-7046

Igama leMchiza:

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

Ikhowudi yoncumo:

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

Ikhowudi ye-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

Isitshixo se-InChi:

MKLKAQMPKHNQPR-NSHDSACASA-N

Igama elingundoqo:

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

Ukunyibilika:Inyibilika kwi-DMSO

Ugcino:0 - 4°C ixesha elifutshane (iintsuku ukuya kwiiveki), okanye -20°C ixesha elide (iinyanga).

Inkcazo:

Kwimodeli ye-tumor ye-CT-26, inhlanganisela ye-E7046 / RT ibangela impendulo yememori ye-anti-tumor yezilwanyana ezili-9. Kwimodeli ye-4T1, indibaniselwano ye-E7046 kunye ne-RT iphinda ivelise umsebenzi ongcono wokuthintela ukukhula kwethumba xa kuthelekiswa nonyango ngalunye lodwa. Indibaniselwano iphucula kakhulu ukuphila ngokuthintela i-metastasis yemiphunga ezenzekelayo ye-4T1 tumors[1]. I-E7046 (150 mg / kg) inqanda ukukhula kweemodeli ezininzi ze-sygeneic tumor. Ukuvalwa kokubonisa i-EP4 kukhuthaza ukuhlukana kwe-anti-tumor DC kwaye kunciphisa ukukhula kwethumba kwiigundane. Unyango lwe-E7046 lunciphisa ukukhula okanye lwaliwe amathumba asekiweyo kwi-vivo ngendlela exhomekeke kuzo zombini iiseli ze-myeloid kunye ne-CD8C T. Ngaphaya koko, ulawulo oluhlangeneyo lwe-E7046 kunye ne-E7777, i-IL-2-diphtheria ye-toxin fusion protein ekhetha ngokubulala i-Tregs, iphazamisa i-myeloid kunye ne-Treg uthungelwano lwe-immunosuppressive, okukhokelela kwiimpendulo ezisebenzayo kunye nezizinzileyo zokulwa ne-tumor kwiimodeli zethumba le mouse [2] .

Ithagethi: EP4