[CAS NO. 1369489-71-3] Palupiprant

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PRODUCTS SPECIFICATIONS [1369489-71-3]

Catalog

HY-103088

Brand

MCE

CAS

1369489-71-3

DESCRIPTION [1369489-71-3]

Overview

MDL	MFCD30502665
Molecular Weight	483.39
Molecular Formula	C22H18F5N3O4
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

For research use only. We do not sell to patients.

Summary

E7046 is an orally bioavailable and specific EP4 antagonist, with IC ₅₀ of 13.5 nM and K _i of 23.14 nM. E7046 exhibits anti-tumor activities ^[1] ^[2] .

IC50 & Target

IC50: 13.5 nM (EP4) ^[2]
Ki: 23.14 nM (EP4) ^[2]

In Vitro

E7046 reverses the immunosuppressive effects of PGE2 on activation and differentiation of human myeloid cells through selective EP4 antagonism ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In the CT-26 tumor model, the E7046/RT combination causes the anti-tumor memory response of 9 animals. In the 4T1 model, the combination of E7046 and RT also produces significant better tumor growth inhibition activity compared with each treatment alone. The combination significantly improves survival by inhibiting the subsequent spontaneous lung metastasis of 4T1 tumors ^[1] . E7046 (150 mg/kg) inhibits the growth of multiple syngeneic tumor models. Blockade of EP4 signaling promotes anti-tumor DC differentiation and slows tumor growth in mice. E7046 treatment reduces the growth or even rejected established tumors in vivo in a manner dependent on both myeloid and CD8C T cells. Furthermore, co-administration of E7046 and E7777, an IL-2-diphtheria toxin fusion protein that preferentially kills Tregs, synergistically disrupts the myeloid and Treg immunosuppressive networks, resulting in effective and durable anti-tumor immune responses in mouse tumor models ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03152370	Adlai Nortye Biopharma Co., Ltd.	Neoadjuvant Therapy in Rectal Cancer	May 17, 2017	Phase 1
NCT02540291	Eisai Inc.	Tumors	July 30, 2015	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 206.87 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0687 mL	10.3436 mL	20.6872 mL
5 mM	0.4137 mL	2.0687 mL	4.1374 mL
10 mM	0.2069 mL	1.0344 mL	2.0687 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.30 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.30 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.30 mM); Clear solution

* All of the co-solvents are available by MCE.