AMX12006

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

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

AMX12006 Chemical Structure

CAS No. : 2639775-01-0

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Biological Activity
Purity & Documentation
References
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Description

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)

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
T_max (h)		0.5
C_max (ng/mL)	4627 ± 304	8243 ± 370
AUC_(0-t)(h·ng/mL)	3375 ± 477	25672 ± 5668
AUC_0–∞ (h·ng/mL)	3416 ± 495	25707 ± 5682
T_1/2(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.

Molecular Weight

481.47

Formula

C₂₆H₂₂F₃N₃O₃

CAS No.

2639775-01-0

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Debasis Das, et al. Discovery of Novel, Selective Prostaglandin EP4 Receptor Antagonists with Efficacy in Cancer Models. ACS Med. Chem. Lett. 2023.

AMX12006 Related Classifications

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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.

Keywords:

AMX120062639775-01-0AMX 12006AMX-12006Prostaglandin Receptororally activecytotoxicantitumorCT-26 cellsInhibitorinhibitorinhibit

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