E-7046

Igama Lekhemikhali:

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

Ikhodi ye-SMILES:

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

Ikhodi ye-InChi:

I-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

I-InChi Key:

I-MKLKAQMPKHNQPR-NSHDSACASA-N

Igama elingukhiye:

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

Ukunyibilika:I-Soluble ku-DMSO

Isitoreji:0 - 4°C isikhathi esifushane (izinsuku ukuya emavikini), noma -20°C isikhathi eside (izinyanga).

Incazelo:

Kumodeli ye-tumor ye-CT-26, inhlanganisela ye-E7046/RT ibangela ukusabela kwenkumbulo ye-anti-tumor yezilwane eziyi-9. Kumodeli ye-4T1, inhlanganisela ye-E7046 ne-RT iphinde ikhiqize umsebenzi obalulekile ongcono wokuvimbela ukukhula kwesimila uma kuqhathaniswa nokwelashwa ngakunye kuphela. Inhlanganisela ithuthukisa kakhulu ukusinda ngokuvimbela i-metastasis yamaphaphu ezenzakalelayo elandelayo yamathumba e-4T1[1]. I-E7046 (150 mg/kg) ivimbela ukukhula kwamamodeli amaningi e-sygeneic tumor. Ukuvinjwa kokusayina kwe-EP4 kukhuthaza ukuhlukaniswa kwe-anti-tumor DC futhi kunciphisa ukukhula kwesimila kumagundane. Ukwelashwa kwe-E7046 kunciphisa ukukhula noma ngisho nezimila ezinqatshiwe ezimisiwe ku-vivo ngendlela encike kuwo womabili amaseli e-myeloid kanye ne-CD8C T. Ngaphezu kwalokho, ukuphathwa ngokubambisana kwe-E7046 ne-E7777, iphrotheni ye-IL-2-diphtheria toxin fusion ekhethela ukubulala i-Tregs, iphazamisa ngokuhlanganyela amanethiwekhi e-myeloid kanye ne-Treg immunosuppressive, okuholela ekuphenduleni okuphumelelayo nokuhlala isikhathi eside kwe-anti-tumor kumamodeli we-tumor yegundane[2] .

Ithagethi: EP4