RO2468

Protein target name:

MDM2

Mechanism of action:

Antagonist

Probe Information

Target and Probe Information

Target Details

Target class:

ACTFS, HDMX, hdm5

Probe Details

Chemical Probes Portal ID:

CPP1595

PubChem CID:

56941948

ChEMBL ID:

CHEMBL3109042

SMILES string:

CC(C)(C)C[C@H]1[C@@]2([C@H]([C@@H](N1)C(=O)NC3=C(C=C(C=C3)C(=O)N)OC)C4=C(C(=CC=C4)Cl)F)C5=CN=C(C=C5NC2=O)Cl

InChi Key:

CGCOPBXAGSCZNX-FNQJWKMRSA-N

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50

6 nM

Potency assay:

HTRF assay.

Structure-activity relationship:

Yes, see ACS Med Chem Lett paper

In cell validation

On target activity in cells

Potency in cells:

IC50

0.015 uM

Potency assay (cells):

Average anti-proliferative activity across multiple p53-positive cell lines (SJSA-1, HCT-116, RKO). RO2468 was 742-fold more potent against p53 wild-type than p53-mutant cell types.

In vivo validation

Organism:

Male C57 mice, Female nude mice

Dose:

5 mg/kg (oral), 2 mg/kg (IV)

Route of delivery:

IntravenousOral

Plasma half life:

3 h (IV)

Systemic clearance:

1,8 mL/min/kg (IV)

Cmax:

2.1 ug/mL (oral)

Organ of Interest

Organ (O):

SJSA-1 xenografts (nude mice, 3-20 mg/kg)

Primary Reference

Reference (doi):

10.1021/ml400359z

Reference (PMID):

24900784

RO2468

Probe Information

Target Details

ACTFS, HDMX, hdm5

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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RO2468

Probe Information

Target Details

ACTFS, HDMX, hdm5

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?