(±)-Nutlin-3
- Catalog NO.:A861337
- CAS No. : 548472-68-0
- Molecular Formula:C30H30Cl2N4O4
- Molecular Weight: 581.49
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Product Details
CAS Number | 548472-68-0 | Appearance | White powder |
Catalog Number | A861337 | MDL Number | MFCD07784509 |
Molecular Formula | C30H30Cl2N4O4 | Molecular Weight | 581.49 |
Boiling Point | Melting Point | ||
Flash Point | Density | ||
Synonyms | RG7112;R7112;rel-4-((4R,5S)-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one | ||
Storage Condition | Store in a tightly closed container,in a cool and dry place |
Safety
GHS Pictogram | |||
Signal Word | Warning | UN Number | |
Hazard Statements | H315-H319-H335 | Class | |
Precautionary Statements | P261-P305+P351+P338 | Packing Group |
Description
Nutlin-3 treatment induces the expression of MDM2 and p21, and displays potent antiproliferative activity with IC50 of ~1.5 μM, only in cells with wild-type p53 such as HCT116, RKO and SJSA-1, but not in the mutant p53 cell lines SW480 and MDA-MB-435. In SJSA-1 cells, Nutlin-3 treatment at 10 μM for 48 hours significantly induces caspase-dependent cell apoptosis by ~45%. Although Nutlin-3 also inhibits the growth and viability of human skin (1043SK) and mouse embryo (NIH/3T3) with IC50 of 2.2 μM and 1.3 μM, respectively, cells remain viable 1 week post-treatment even at 10 μM of Nutlin-3, in contrast with the SJSA-1 cells with viability lost at 3 μM of Nutlin-3 treatment.Nutlin-3 does not induce the phosphorylation of p53 on key serine residues and reveals no difference in their sequence-specific DNA binding and ability to transactivate p53 target genes compared with phosphorylated p53 induced by the genotoxic drugs doxorubicin and etoposide, demonstrating that phosphorylation of p53 o |