Formulation: A solid
Formal Name: (6S)-5-(5-chloro-1,2-dihydro-1-methyl-2-oxo-3-pyridinyl)-6-(4-chlorophenyl)-2-(2,4-dimethoxy-5-pyrimidinyl)-5,6-dihydro-1-(1-methylethyl)-pyrrolo[3,4-d]imidazol-4(1H)-one
Purity: ≥98%
Formula Markup: C26H24Cl2N6O4
Formula Weight: 555,4
Shelf life (days): 1460
CAS Number: 1448867-41-1
Notes: Siremadlin is an inhibitor of the protein-protein interaction between the E3 ubiquitin ligase MDM2 and p53 (IC50 = 0.21 nM).{68355} It selectively inhibits the MDM2-p53 protein-protein interaction over MDM4-p53, YAP1-TEAD4, PCSK9-LDLR, and Bcl-2-Bak interactions in time-resolved FRET (TR-FRET) assays (IC50s = 3.3, >150, >50, and >50 µM, respectively). Siremadlin inhibits the growth of SJSA-1 osteosarcoma cells (GI50 = 38 nM). It also induces apoptosis in SJSA-1 cells when used at a concentration of 100 nM. In vivo, siremadlin (27 mg/kg) induces tumor regression and prevents tumor regrowth in an SJSA-1 rat xenograft model and an HSAX2655 patient-derived xenograft (PDX) rat liposarcoma model.
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