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Art. -Nr.: HY-100765

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BI-0252

BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC₅₀ of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.

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CAS. Nr.: 1818291-27-8
Formel: C₃₀H₂₆Cl₂FN₃O₃
Molecular Weight:566.45

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (279 KB)

BI-0252 Chemical Structure

CAS. Nr.: 1818291-27-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 4 nM (MDM2-p53)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
SJSA-1	IC₅₀	471 nM Compound: 3; BI-0252	Antiproliferative activity against human SJSA-1 cells expression wild type p53 incubated for 3 days by Alamar Blue dye based assay Antiproliferative activity against human SJSA-1 cells expression wild type p53 incubated for 3 days by Alamar Blue dye based assay	[PMID: 27775892]
SK-OV-3	IC₅₀	>25000 nM Compound: 3; BI-0252	Antiproliferative activity against human SK-OV-3 cells expression p53 mutant incubated for 3 days by Alamar Blue dye based assay Antiproliferative activity against human SK-OV-3 cells expression p53 mutant incubated for 3 days by Alamar Blue dye based assay	[PMID: 27775892]

In Vivo

BI-0252 (orally; 25 mg/kg/day for 13 days and 100 mg/kg for 24 h) leads to time-dependent mRNA induction of TP53 target genes including CDKN1a, MDM2, and BBC3^[1].
BI-0252 (iv and po; an iv dose of 5 mg/kg and a po dose of 50 mg/kg) showes low clearance in vivo after iv administration and high clearance after po administration. BI-0252 has high po in vivo exposure and good cellular potency^[1].

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

Animal Model:

Nude mice bearing established subcutaneous SJSA-1 tumors^[1]
Dosage:

25 mg/kg/day or a single dose of 100 mg/kg
Administration:

Orally; 25 mg/kg/day for 13 days and 100 mg/kg for 24 hours
Result:

Leaded to time-dependent mRNA induction of TP53 target genes.

Animal Model:

Nontumor-bearing female NMRI nude mice^[1]
Dosage:

An iv dose of 5 mg/kg and a po dose of 50 mg/kg
Administration:

Iv and po
Result:

Showed low clearance in vivo after iv administration and high clearance after po administration.

Chemical Information

CAS. Nr. 1818291-27-8
Molecular Weight 566.45
Formel C₃₀H₂₆Cl₂FN₃O₃
SMILES

ClC1=C(F)C([C@@H]2[C@@]3(C(C=CC(Cl)=C4)=C4NC3=O)N(CC5CC5)[C@@H]6[C@H]2N[C@@H](C7=CC=C(C(O)=O)C=C7)C6)=CC=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Gollner A, et al. Discovery of Novel Spiro[^[3]H-indole-3,2'-pyrrolidin]-2(1H)-one Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2-p53 Interaction. J Med Chem. 2016 Nov 23;59(22):10147-10162. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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