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

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.

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Brigimadlin

Brigimadlin Chemical Structure

CAS No. : 2095116-40-6

Size Prix Stock Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
1 mg En stock
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg En stock
200 mg   Obtenir un devis  
500 mg   Obtenir un devis  

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Other Forms of Brigimadlin:

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-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.
Essai clinique
Masse moléculaire

591.46

Formule

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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
In Vitro: 

DMSO : 50 mg/mL (84.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6907 mL 8.4537 mL 16.9073 mL
5 mM 0.3381 mL 1.6907 mL 3.3815 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (2.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.25 mg/mL (2.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation

Purity: 99.88%

SDS (644 KB)

COA (258 KB) HNMR (387 KB) RP-HPLC (253 KB) LCMS (95 KB)

Instruction de manipulation (2659 KB)
Références

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6907 mL 8.4537 mL 16.9073 mL 42.2683 mL
5 mM 0.3381 mL 1.6907 mL 3.3815 mL 8.4537 mL
10 mM 0.1691 mL 0.8454 mL 1.6907 mL 4.2268 mL
15 mM 0.1127 mL 0.5636 mL 1.1272 mL 2.8179 mL
20 mM 0.0845 mL 0.4227 mL 0.8454 mL 2.1134 mL
25 mM 0.0676 mL 0.3381 mL 0.6763 mL 1.6907 mL
30 mM 0.0564 mL 0.2818 mL 0.5636 mL 1.4089 mL
40 mM 0.0423 mL 0.2113 mL 0.4227 mL 1.0567 mL
50 mM 0.0338 mL 0.1691 mL 0.3381 mL 0.8454 mL
60 mM 0.0282 mL 0.1409 mL 0.2818 mL 0.7045 mL
80 mM 0.0211 mL 0.1057 mL 0.2113 mL 0.5284 mL
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Brigimadlin Related Classifications

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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