E-7046

Orukọ Kemikali:

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

KỌỌDỌ 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

Koodu 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

Bọtini InChi:

MKLKAQMPKHNQPR-NSHDSACASA-N

Koko-ọrọ:

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

Solubility:Tiotuka ni DMSO

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

Apejuwe:

Ninu awoṣe tumo CT-26, apapo E7046/RT fa idahun iranti iranti egboogi-egbo ti awọn ẹranko 9. Ninu awoṣe 4T1, apapọ E7046 ati RT tun ṣe agbejade iṣẹ ṣiṣe idinamọ idagbasoke tumo to dara julọ ni akawe pẹlu itọju kọọkan nikan. Ijọpọ naa ṣe imudara iwalaaye ni pataki nipa didaduro metastasis ẹdọfóró lẹẹkọkan ti awọn èèmọ 4T1[1]. E7046 (150 mg/kg) ṣe idiwọ idagbasoke ti awọn awoṣe tumo syngeneic pupọ. Blockade ti ifihan ifihan EP4 n ṣe agbega iyatọ anti-tumor DC ati fa fifalẹ idagbasoke tumo ninu awọn eku. Itọju E7046 dinku idagba tabi paapaa kọ awọn èèmọ ti iṣeto ni vivo ni ọna ti o da lori mejeeji myeloid ati awọn sẹẹli CD8C T. Pẹlupẹlu, iṣakoso iṣakoso ti E7046 ati E7777, amuaradagba IL-2-diphtheria toxin fusion protein ti o fẹ pa Tregs, synergistically disrupts myeloid and Treg immunosuppressive nẹtiwọki, Abajade ni munadoko ati ki o tọ egboogi-tumo idahun esi ni Asin tumo si dede[2] .

afojusun: EP4