E-7046

Ingoa matū:

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

Waehere 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

Waehere 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

Kī InChi:

MKLKAQMPKHNQPR-NSHDSACASA-N

Kupumatua:

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

Wairewa:Wairewa i roto i te DMSO

Rokiroki:0 - 4°C mo te wa poto (ra ki nga wiki), -20°C ranei mo te wa roa (marama).

Whakaahuatanga:

I roto i te tauira pukupuku CT-26, ko te huinga E7046/RT ka puta te whakautu mahara anti-tumor o nga kararehe 9. I roto i te tauira 4T1, ko te whakakotahitanga o te E7046 me te RT ka nui ake te pai ake o te mahi aukati i te tipu o te puku ina whakaritea ki ia maimoatanga anake. Ko te whakakotahitanga ka tino whakapai ake i te oranga ma te aukati i te metastasis o te pukahukahu o muri mai o nga pukupuku 4T1[1]. Ko te E7046 (150 mg / kg) ka aukati i te tipu o nga tauira pukupuku syngeneic maha. Ko te aukati o te tohu tohu EP4 e whakatairanga ana i te rereketanga o te DC anti-tumor me te whakaroa i te tipu o te pukupuku i roto i nga kiore. Ko te maimoatanga E7046 ka whakaiti i te tipu, ka paopao ranei i nga pukupuku kua whakapumautia i roto i te vivo i runga i nga tikanga e whakawhirinaki ana ki nga pūtau myeloid me te CD8C T. I tua atu, ko te whakahaere tahi o te E7046 me te E7777, he IL-2-diphtheria toxin fusion pūmua e pai ana ki te patu i a Tregs, ka whakaporearea i te myeloid me te Treg whatunga immunosuppressive, ka puta mai he urupare aukati anti-tumor i roto i nga tauira pukupuku kiore [2] .

Whāinga: EP4