1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. AMX12006

AMX12006 is a potent, selective and orally active EP4 antagonist with an IC50 value of 4.3 nM. AMX12006 shows cytotoxic and antitumor activity.

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AMX12006

AMX12006 Chemische Struktur

CAS. Nr. : 2639775-01-0

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Beschreibung

AMX12006 is a potent, selective and orally active EP4 antagonist with an IC50 value of 4.3 nM. AMX12006 shows cytotoxic and antitumor activity[1].

IC50 & Target[1]

hEP4

4.3 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
4T1 IC50
79.47 μM
Compound: 36; AMX12006
Cytotoxicity against mouse 4T1 cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
Cytotoxicity against mouse 4T1 cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
[PMID: 37312837]
CT26.WT IC50
41.39 μM
Compound: 36; AMX12006
Cytotoxicity against mouse CT26.WT cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
Cytotoxicity against mouse CT26.WT cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
[PMID: 37312837]
Lewis lung carcinoma cell line IC50
>100 μM
Compound: 36; AMX12006
Cytotoxicity against mouse Lewis lung carcinoma cell line assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
Cytotoxicity against mouse Lewis lung carcinoma cell line assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
[PMID: 37312837]
MCF7 IC50
46.73 μM
Compound: 36; AMX12006
Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by Cell-titer glo assay
[PMID: 37312837]
In Vitro

AMX12006 (compound 36) (0-100 µM) shows cytotoxic with IC50s of 46.73, 79.47, >100, 41.39, >100 µM for MCF-7, 4T1, HCA-7, CT-26 WT, LLC cells, respectively[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7, 4T1, HCA-7, CT-26 WT, LLC cells
Concentration: 0-100 µM
Incubation Time:
Result: Showed cytotoxic with IC50s of 46.73, 79.47, >100, 41.39, >100 µM for MCF-7, 4T1, HCA-7, CT-26 WT, LLC cells, respectively.
In Vivo

AMX12006 (75, 150 mg/kg; p.o.; once daily for 11 days) shows antitumor activity in a dose-dependent manner[1].
Pharmacokinetic Parameters of AMX12006 in Sprague-Dawley rats[1].

iv, 1 mg/kg po, 10 mg/kg
Tmax (h) 0.5
Cmax (ng/mL) 4627 ± 304 8243 ± 370
AUC(0-t)(h·ng/mL) 3375 ± 477 25672 ± 5668
AUC0–∞ (h·ng/mL) 3416 ± 495 25707 ± 5682
T1/2(h) 1.4 ± 0.3 2.7 ± 0.2
CL (mL/min/kg) 4.95 ± 0.77
Vdss (L/kg) 0.41 ± 0.04
F % 76.1
Sprague-Dawley rats, 1 mg/kg iv ; 10 mg/kg po[1]

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

Molekulargewicht

481.47

Formel

C26H22F3N3O3

CAS. Nr.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(N[C@@H](C)C1=CC=C(C(O)=O)C=C1)C2=C(C3=CC=CC=C3N2C)NC4=CC(C(F)(F)F)=CC=C4

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMF : 20 mg/mL (41.54 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0770 mL 10.3849 mL 20.7697 mL
5 mM 0.4154 mL 2.0770 mL 4.1539 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation

Purity: 99.9%

Verweise

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMF 1 mM 2.0770 mL 10.3849 mL 20.7697 mL 51.9243 mL
5 mM 0.4154 mL 2.0770 mL 4.1539 mL 10.3849 mL
10 mM 0.2077 mL 1.0385 mL 2.0770 mL 5.1924 mL
15 mM 0.1385 mL 0.6923 mL 1.3846 mL 3.4616 mL
20 mM 0.1038 mL 0.5192 mL 1.0385 mL 2.5962 mL
25 mM 0.0831 mL 0.4154 mL 0.8308 mL 2.0770 mL
30 mM 0.0692 mL 0.3462 mL 0.6923 mL 1.7308 mL
40 mM 0.0519 mL 0.2596 mL 0.5192 mL 1.2981 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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AMX12006
Art. -Nr.:
HY-149290
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