E7046 is a potent and selective antagonist of the type 4 prostaglandin E2 (PGE2) receptor EP4. EP4 Antagonism by E7046 diminishes Myeloid immunosuppression and synergizes with Treg-reducing IL-2-Diphtheria toxin fusion protein in restoring anti-tumor immunity. E7046 has specific and potent inhibitory activity on PGE2-mediated pro-tumor myeloid cell differentiation and activation. E7046 treatment reduced the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8+ T cells.
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Name | E7046 |
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Iupac Chemical Name | 4-[(1S)-1-[[[3-(difluoromethyl)-1-methyl-5-[3-(trifluoromethyl)phenoxy]-1H-pyrazol-4-yl]carbonyl]amino]ethyl]-benzoic acid |
Synonyms | E7046; E-7046; E 7046. |
Molecular Formula | C22H18F5N3O4 |
Molecular Weight | 483.39 |
Smile | 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 |
InChiKey | MKLKAQMPKHNQPR-NSHDSACASA-N |
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 |
CAS Number | 1369489-71-3 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
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Bulk | Enquiry | Enquiry | Enquiry |
Formulation | Off-white solid |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
Solubility | Soluble in DMSO |
Handling | Refer to MSDS |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
HS Code | 2934200090 |
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Clinical study |
1: Albu DI, Wang Z, Huang KC, Wu J, Twine N, Leacu S, Ingersoll C, Parent L, Lee W, Liu D, Wright-Michaud R, Kumar N, Kuznetsov G, Chen Q, Zheng W, Nomoto K, Woodall-Jappe M, Bao X. EP4 Antagonism by E7046 diminishes Myeloid immunosuppression and synergizes with Treg-reducing IL-2-Diphtheria toxin fusion protein in restoring anti-tumor immunity. Oncoimmunology. 2017 Jun 28;6(8):e1338239. doi: 10.1080/2162402X.2017.1338239. eCollection 2017. PubMed PMID: 28920002; PubMed Central PMCID: PMC5593700.
2: Wan J, Zhang L, Lu G, Gu W, Huang L, Ge L, Zhang X, Ji L, Chen Q, Di R, Jiang Y. Midterm outcomes of intracranial aneurysms with bleb formation with densely coiling of the aneurismal neck or entire aneurysm. Medicine (Baltimore). 2017 Aug;96(33):e7046. doi: 10.1097/MD.0000000000007046. PubMed PMID: 28816934; PubMed Central PMCID: PMC5571671.
3: Noroozi Karimabad M, Hassanshahi G, Arababadi MK. Controversial report regarding seroprevalence of hepatitis B and C viruses among hemodialysis patients in kerman province, South-East iran. Hepat Mon. 2013 Mar 13;13(3):e7046. doi: 10.5812/hepatmon.7046. Print 2013 Mar. PubMed PMID: 23675385; PubMed Central PMCID: PMC3651842.
4: Gustafsson MC, Knight D, Palmer CN. Ligand modulated antagonism of PPARgamma by genomic and non-genomic actions of PPARdelta. PLoS One. 2009 Sep 16;4(9):e7046. doi: 10.1371/journal.pone.0007046. PubMed PMID: 19756148; PubMed Central PMCID: PMC2737640.