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Art. -Nr.: HY-12737

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AM-6761

AM-6761 is a potent MDM2 inhibitor with an IC₅₀ of 0.1 nM.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 1584732-36-4
Formel: C₃₃H₃₇Cl₂FN₂O₅S₂
Molecular Weight:695.69

Speicherung:

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

Data Sheet (279 KB)

AM-6761 Chemical Structure

CAS. Nr.: 1584732-36-4

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

AM-6761 is a potent MDM2 inhibitor with an IC₅₀ of 0.1 nM.

IC₅₀ & Target

IC50: 0.1 nM (MDM2)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	11 nM Compound: 4, AM-6761	Cytotoxicity against human HCT116 cells expressing p53 assessed as growth inhibition after 16 hrs by flow cytometry-based BrdU incorporation assay in presence of 10% human serum Cytotoxicity against human HCT116 cells expressing p53 assessed as growth inhibition after 16 hrs by flow cytometry-based BrdU incorporation assay in presence of 10% human serum	[PMID: 24601644]
HCT-116	IC₅₀	58 nM Compound: 4, AM-6761	Binding affinity to MDM2 in human HCT116 cells expressing p53 assessed as upregulation of p21 mRNA expression after 7 hrs by quantitative RT-PCR analysis Binding affinity to MDM2 in human HCT116 cells expressing p53 assessed as upregulation of p21 mRNA expression after 7 hrs by quantitative RT-PCR analysis	[PMID: 24601644]
SJSA-1	ED₅₀	11 mg/kg Compound: 4, AM-6761	Antitumor activity against human SJSA1 cells xenografted in po dosed Harlan athymic nude mouse assessed as tumor growth inhibition at 25 mg/kg, administered as qd on day 9 post tumor implantation measured twice per week Antitumor activity against human SJSA1 cells xenografted in po dosed Harlan athymic nude mouse assessed as tumor growth inhibition at 25 mg/kg, administered as qd on day 9 post tumor implantation measured twice per week	[PMID: 24601644]
SJSA-1	IC₅₀	16 nM Compound: 4, AM-6761	Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum	[PMID: 24601644]

In Vitro

AM-6761 is a potent inhibitor with remarkable biochemical (IC₅₀=0.1 nM) and cellular potency (IC₅₀=16 nM)^[1].

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

In Vivo

AM-6761 has favorable pharmacokinetic properties.AM-6761 shows excellent antitumor activity in the SJSA-1 osteosarcoma xenograft model with an ED₅₀ of 11 mg/kg^[1].

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

Chemical Information

CAS. Nr. 1584732-36-4
Molecular Weight 695.69
Formel C₃₃H₃₇Cl₂FN₂O₅S₂
SMILES

O=C(O)CC1=CN=C(C[C@]2(C)C(N([C@@H](C3CC3)CS(=O)(C(C)(C)C)=O)[C@H](C4=CC=C(Cl)C(F)=C4)[C@@H](C5=CC=CC(Cl)=C5)C2)=O)S1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Gonzalez AZ, et al. Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres. J Med Chem. 2014 Apr 10;57(7):2963-88. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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