An inhibitor of the p53-MDM2 protein-protein interaction
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BI-907828

Item No. 44353

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2′S,3′S, 3′aS,10′aS)-6-chloro-3′-(3-chloro-2-fluorophenyl)-1′-(cyclopropylmethyl)-1,2,3′,3′a,10′,10′a-hexahydro-6′-methyl-2-oxo-spiro[3H-indole-3,2′(1′H)-pyrrolo[2′,3′:4,5]pyrrolo[1,2-b]indazole]-7′carboxylic acid
CAS Number
2095116-40-6
Synonyms
  • Brigimadlin
Molecular Formula
C31H25Cl2FN4O3
Formula Weight
591.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
OC(C1=C(C)C2=NN([C@@]([C@]3([H])C4)([H])[C@H](C5=C(C(Cl)=CC=C5)F)[C@@]6(C7=CC=C(Cl)C=C7NC6=O)N3CC8CC8)C4=C2C=C1)=O
InChi Code
InChI=1S/C31H25Cl2FN4O3/c1-14-17(29(39)40)8-9-18-23-12-24-28(38(23)36-27(14)18)25(19-3-2-4-21(33)26(19)34)31(37(24)13-15-5-6-15)20-10-7-16(32)11-22(20)35-30(31)41/h2-4,7-11,15,24-25,28H,5-6,12-13H2,1H3,(H,35,41)(H,39,40)/t24-,25-,28+,31+/m0/s1
InChi Key
AMTXDBGKYPDTTA-SJVQGLCSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $47

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    5 mg

    $223

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    10 mg

    $400

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    25 mg

    $646

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    Cayman Chemical
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    Product Description

    BI-907828 is an inhibitor of the protein-protein interaction between p53 and murine double minute 2 (MDM2; IC50 = 2 nM in a cell-free assay).1 It is selective for the p53-MDM2 interaction over the p53-MDMX interaction (IC50 = 7,944 nM). BI-907828 selectively inhibits the proliferation of Colon-26 colon cancer cells, which express wild-type p53, over 4T1 breast and MC-38 colon cancer cells, which express mutant p53 (IC50s = 259, 5,579, and 9,782 nM, respectively). It inhibits the proliferation of SJSA-1 osteosarcoma cells, BJ human foreskin fibroblasts, and hTERT RPE-1 retinal pigment epithelial cells but only induces apoptosis in SJSA-1 cells. BI-907828 induces tumor regression in an SJSA-1 mouse xenograft model and patient-derived xenograft (PDX) models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gollner, A., Rudolph, D., Weyer-Czernilofsky, U., et al. Discovery and characterization of brigimadlin, a novel and highly potent MDM2-p53 antagonist suitable for intermittent dose schedules. Mol. Cancer Ther. 23(12), 1689-1702 (2024).