An inhibitor of the MDM2-p53 protein-protein interaction
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Product Categories

Product Type

Biochemicals

Research Area

Cancer
Cell Death
Apoptosis
Transcription Factors
p53

Siremadlin

Item No. 38516

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
CAS Number
1448867-41-1
Synonyms
  • HDM201
  • NVP-HDM201
Molecular Formula
C26H24Cl2N6O4
Formula Weight
555.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 10 mg/mlEthanol: 15 mg/ml
λmax
223, 336 nm
SMILES
ClC1=CC=C([C@@H]2N(C(C3=C2N(C(C)C)C(C4=CN=C(N=C4OC)OC)=N3)=O)C5=CC(Cl)=CN(C5=O)C)C=C1
InChi Code
InChI=1S/C26H24Cl2N6O4/c1-13(2)33-21-19(30-22(33)17-11-29-26(38-5)31-23(17)37-4)25(36)34(18-10-16(28)12-32(3)24(18)35)20(21)14-6-8-15(27)9-7-14/h6-13,20H,1-5H3/t20-/m0/s1
InChi Key
AGBSXNCBIWWLHD-FQEVSTJZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $32

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    5 mg

    $104

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    10 mg

    $192

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    25 mg

    $400

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    Cayman Chemical
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    Product Description

    Siremadlin is an inhibitor of the protein-protein interaction between the E3 ubiquitin ligase MDM2 and p53 (IC50 = 0.21 nM).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jeay, S., Ferretti, S., Holzer, P., et al. Dose and schedule determine distinct molecular mechanisms underlying the efficacy of the p53-MDM2 inhibitor HDM201. Cancer Res. 78(21), 6257-6267 (2018).