General
Preferred name
SAR-405838
Synonyms
SAR405838 ()
MI-773 ()
MI-77301 ()
MI-773 (SAR405838) ()
Sar 405838 ()
P&D ID
PD021549
CAS
1303607-60-4
Tags
available
probe
drug candidate
Drug Status
investigational
Max Phase
1.0
Drug indication
Neoplasm
Probe info
Probe type
P&D approved
experimental probe
Probe selectivity
protein-selective
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
35
No orthogonal probes found
Similar probes
4
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
COMMENT
MI-77301 (synonym SAR405838) is a highly potent and selective MDM2 inhibitor (Ki=0.88 nM). MI-77301 inhibits the cell growth of cancer cell lines like p53 wild-type osteosarcoma SJSA-1 cell line (IC50=92 nM). The in vivo efficacy of the compound was shown in particular in the SJSA-1 osteosarcoma xenograft model. Aug 9 2017 - 1:48pm; This probe is the result of extensive chemistry optimization over the last 10 years. The original compound was a rationally designed inhibitor of the interaction between p53 and MDM2, but it had liabilities that prevented clinical development. This latest compound appears to be outstanding in both cells and a variety of mouse xenograft cancer models. Aug 18 2017 - 4:27pm
PRICE
243
DESCRIPTION
MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
MOA
Antagonist
(Chemical Probes.org)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
4
Organisms
0
Compound Sets
9
Axon Medchem Screening Library
ChEMBL Drugs
Chemical Probes.org
Drug Repurposing Hub
DrugBank
High-quality chemical probes
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
21
Molecular Weight
561.2
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
4
Rotatable Bonds
4
Ring Count
5
Aromatic Ring Count
2
cLogP
5.3
TPSA
90.46
Fraction CSP3
0.52
Chiral centers
4.0
Largest ring
6.0
QED
0.41
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
MDM2
MDM2 inhibitor
Apoptosis
E1/E2/E3 Enzyme
MDM-2/p53
MDM2/MDMX,p53
MOA
MDM inhibitor
Orthogonal probe
RO5353
Pathway
Metabolic Enzyme/Protease
Target class
Other post-translational modification
Target subclass
E3 ubiquitin ligase
Source data
