2. Metabolic Enzyme/Protease Apoptosis
  3. E1/E2/E3 Enzyme MDM-2/p53
  4. Brigimadlin

Brigimadlin  (Synonyms: BI 907828)

Cat. No.: HY-152859 Purity: 98.96% ee.: 100%
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Brigimadlin (BI 907828) is an orally active E3 ubiquitin-protein ligase MDM-2 inhibitor, preventing MDM-2 from negatively regulating the tumor suppressor p53. Brigimadlin can be used for antineoplastic research.

For research use only. We do not sell to patients.

Brigimadlin Chemical Structure

Brigimadlin Chemical Structure

CAS No. : 2095116-40-6

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1 mg USD 620 In-stock
5 mg USD 1230 In-stock
10 mg USD 1960 In-stock
25 mg USD 3620 In-stock
50 mg USD 5450 In-stock
100 mg USD 8200 In-stock
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Based on 1 publication(s) in Google Scholar

Brigimadlin Related Antibodies

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Description

Brigimadlin (BI 907828) is an orally active E3 ubiquitin-protein ligase MDM-2 inhibitor, preventing MDM-2 from negatively regulating the tumor suppressor p53. Brigimadlin can be used for antineoplastic research[1][2][3][4].

In Vitro

Brigimadlin (0-10 nM, 48 h) inhibits viability and induces cell death in brain tumor stem cells (BTSCs)[3].
Brigimadlin (1-50 nM, 48 h) induces apoptosis and increases p53 transcriptional targets (p21 and PUMA) in BT48, BT67, BT73 cells[3].
Brigimadlin (1 nM, 48 h) disrupts the interaction between MDM2 and wild-type p53 in brain tumor stem cells (BTSCs)[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Brigimadlin Related Antibodies

Cell Viability Assay[3]

Cell Line: BT48, BT50, BT67, BT69, BT89, BT94
Concentration: 0-10 nM
Incubation Time: 48 h
Result: IC50: 58.5, 21.1, 37.9, 89.8, 16.7, 46.8 pM.

Western Blot Analysis[3]

Cell Line: BT48, BT67, BT73 cells
Concentration: 0-50 nM
Incubation Time: 48 h
Result: Upregulated p21 and PUMA, and increased cleaved PARP level.
In Vivo

Brigimadlin (15 and 50 mg/kg, p.o., once a week) inhibits tumor growth and increases median survival in orthotopic xenografts of both a MDM2 amplified (BT48) and a normal CN (BT67), TP53 wild-type BTSC model[3].
Brigimadlin (50 mg/kg, p.o., a single dose) increasees PD biomarkers (CDKN1a and GDF15) in the brain in orthotopic GBM patient-derived BTSC models (BT48 and BT67) in SCID mice, and has low systemic clearance[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

591.46

Formula

C31H25Cl2FN4O3
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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Brigimadlin Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Brigimadlin2095116-40-6BI 907828BI907828BI-907828E1/E2/E3 EnzymeMDM-2/p53E1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseBTSCGBMtumorBT48BT67BT73Inhibitorinhibitorinhibit

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