1369489-71-3 Usage
Description
E-7046 is an orally bioavailable and specific EP4 antagonist, which is a type of compound that can inhibit the action of certain receptors in the body. It has been found to exhibit anti-tumor activity, making it a promising candidate for cancer treatment.
Uses
Used in Anticancer Applications:
E-7046 is used as an anti-tumor agent for its ability to reverse PGE2-induced suppression of TNFα production in human whole blood. This suggests that it may be effective in modulating the immune response to cancer and potentially improving the effectiveness of other cancer treatments.
Used in Pharmaceutical Industry:
E-7046 is used as a research compound for the development of new cancer treatments. Its specific action as an EP4 antagonist makes it a valuable tool for studying the role of this receptor in cancer progression and for developing targeted therapies.
Biological Activity
e7046 is a potent and selective antagonist that potently competes with pge2 binding to the type 4 prostaglandin e2 (pge2) receptor ep4 [1,2].prostaglandin e2 receptor 4 (ep4) is a prostaglandin receptor for prostaglandin e2 (pge2) implicated in various physiological and pathological responses in animal models and humans [3].
in vivo
in apcmin/+ mice, daily oral administration of e7046 slowed down the growth of established subcutaneous tumors and significantly delayed the recurrence of tumors after surgical resection. e7046 significantly reduced the combined colon polyp area and the size of individual polyps without influencing the total polyp number. e7046 exhibited great activity against colon and small intestine tumors [1]. e7046 delayed the growth of multiple syngeneic murine tumor types. e7046 showed no effect on tumor cell viability in vitro [2]. in the ct26 model, treatment with e7046 and anti-pd1 inhibited tumor growth. in the 4t1 model, e7046 in combination with anti-ctla4 resulted in a nearly complete tumor growth inhibition [4].
references
[1] albu d i, wu j, huang k, et al. abstract b198: pharmacological profile of the pge2 ep4 receptor antagonist e7046[j]. 2015.[2] albu d i, huang k c, wu j, et al. abstract b034: preclinical immune antitumor activity of myeloid-targeting e7046 and treg depleting e7777[j]. 2016.[3] negishi m, sugimoto y, ichikawa a. prostaglandin e receptors[j]. journal of lipid mediators and cell signalling, 1995, 12(2-3): 379-391.[4] bao x, albu d, huang k c, et al. combination of ep4 antagonist and checkpoint inhibitors promotes anti-tumor effector t cells in preclinical tumor models[j]. journal for immunotherapy of cancer, 2015, 3(2): p350.
Check Digit Verification of cas no
The CAS Registry Mumber 1369489-71-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,6,9,4,8 and 9 respectively; the second part has 2 digits, 7 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1369489-71:
(9*1)+(8*3)+(7*6)+(6*9)+(5*4)+(4*8)+(3*9)+(2*7)+(1*1)=223
223 % 10 = 3
So 1369489-71-3 is a valid CAS Registry Number.
1369489-71-3Relevant articles and documents
PHARMACEUTICAL COMPOSITION
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Page/Page column 33, (2012/04/10)
The present invention provides compounds of Formula (I): along with pharmaceutical compositions containing the same, and methods of use thereof in subjects in need of treatment.
