E-7046

Lub npe tshuaj:

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

SMILES Code:

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

InChi Code:

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

Lo lus tseem ceeb:

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

Solubility:Soluble hauv DMSO

Cia:0 - 4 ° C rau lub sijhawm luv (hnub mus rau lub lis piam), lossis -20 ° C rau lub sijhawm ntev (hli).

Nqe lus piav qhia:

Hauv CT-26 tus qauv qog, E7046 / RT ua ke ua rau cov qog nqaij hlav nco txog 9 tus tsiaj. Hauv 4T1 qauv, kev sib xyaw ua ke ntawm E7046 thiab RT kuj tseem ua rau cov qog loj hlob zoo dua inhibition kev ua haujlwm piv nrog txhua qhov kev kho mob ib leeg. Kev sib xyaw ua ke txhim kho kev ciaj sia los ntawm inhibiting qhov tshwm sim tom qab lub ntsws metastasis ntawm 4T1 cov qog [1]. E7046 (150 mg / kg) inhibits kev loj hlob ntawm ntau hom qog nqaij hlav. Blockade ntawm EP4 signaling txhawb kev tiv thaiv qog DC sib txawv thiab ua rau cov qog loj hlob hauv cov nas. Kev kho E7046 txo qhov kev loj hlob lossis txawm tias tsis lees txais cov qog tsim hauv vivo nyob rau hauv ob qho tib si myeloid thiab CD8C T hlwb. Tsis tas li ntawd, kev sib koom ua ke ntawm E7046 thiab E7777, ib qho IL-2-diphtheria toxin fusion protein uas nyiam tua Tregs, synergistically cuam tshuam cov myeloid thiab Treg immunosuppressive tes hauj lwm, uas ua rau muaj txiaj ntsig zoo thiab ruaj khov tiv thaiv kab mob hauv cov qauv nas[2] .

Lub Hom Phiaj: EP4