RO-5963 , CAS No.1416663-77-8

Item Number
R646304
Grouped product items
SKUSizeAvailabilityPrice Qty
R646304-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$184.90
R646304-5mg
5mg
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$586.90
R646304-10mg
10mg
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$855.90
R646304-25mg
25mg
Available within 8-12 weeks(?)
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$1,425.90

Basic Description

Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Product Description

RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC 50 s of ~17 nM and ~24 nM, respectively

In Vitro

RO-5963 (10-20 μM; 48 hours) shows much higher apoptotic activity than Nutlin in both MCF7 and ZR75-30 cell lines. RO-5963 (10 μM, 24 hours) effectively activats p53 and elevates p21 and MDM2 levels. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: ZR75-30, MCF7 cells Concentration: 10, 20 μM Incubation Time: 48 hours Result: Potently showed apoptotic activity. Western Blot AnalysisCell Line: LNCap, U2OS, RKO, A489, 22Rv1, HCT116, H460, LOX, MCF7, A549, G401 cells Concentration: 10 μM Incubation Time: 24 hour Result: Effectively activated p53 and elevated p21 and MDM2 levels.

Form:Solid

IC50& Target:IC50: ~17 nM (p53-MDM2), ~24 nM (p53-MDMX)

Names and Identifiers

IUPAC Name 2-[5-[(6-chloro-7-methylindol-3-ylidene)methyl]-4-hydroxy-2-oxo-1H-imidazol-3-yl]-2-(3,4-difluorophenyl)-N-(1,3-dihydroxypropan-2-yl)acetamide
INCHI InChI=1S/C24H21ClF2N4O5/c1-11-16(25)4-3-15-13(8-28-20(11)15)7-19-23(35)31(24(36)30-19)21(22(34)29-14(9-32)10-33)12-2-5-17(26)18(27)6-12/h2-8,14,21,32-33,35H,9-10H2,1H3,(H,29,34)(H,30,36)
InChi Key IFYMUYSGUSHEPI-UHFFFAOYSA-N
Canonical SMILES CC1=C(C=CC2=C1N=CC2=CC3=C(N(C(=O)N3)C(C4=CC(=C(C=C4)F)F)C(=O)NC(CO)CO)O)Cl
PubChem CID 136683438
Molecular Weight 518.90

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