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Merck

444145

MDM2 Inhibitor

The MDM2 Inhibitor, also referenced under CAS 562823-84-1, controls the biological activity of MDM2.

Synonym(s):

MDM2 Inhibitor, trans-4-Iodo, 4ʹ-boranyl-chalcone, MDM2 Antagonist IV

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About This Item

Empirical Formula (Hill Notation):
C15H12BIO3
CAS Number:
562823-84-1
Molecular Weight:
377.97
UNSPSC Code:
12352200

Key Documents

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Product Name

MDM2 Inhibitor, The MDM2 Inhibitor, also referenced under CAS 562823-84-1, controls the biological activity of MDM2.

InChI key

BYMGWCQXSPGCMW-XCVCLJGOSA-N

InChI

1S/C15H12BIO3/c17-14-8-1-11(2-9-14)3-10-15(18)12-4-6-13(7-5-12)16(19)20/h1-10,19-20H/b10-3+

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

pale yellow

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

Reversible: no
Target IC50: 10, 8.8, and 7 µM in selective toxicity for MDA-MB-435, MDA-MB-231, and Wt-MCF7, respectively
Cell permeable: yes
Primary Target
MDM2
Product does not compete with ATP.

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)

General description

A cell-permeable boranyl-chalcone compound that binds strongly to MDM2 and irreversibly disrupts MDM2/p53 protein complex formation. Exhibits selective toxicity to MDM2-overexpressing human breast cancer cell lines (IC50 = 10 µM for MDA-MB-435, 8.8 µM for MDA-MB-231, and 7 µM for Wt-MCF7) compared to normal breast cell lines (IC50 = 75 µM for MCF-10A and 63 µM for MCF-12A).
A cell-permeable boranyl-chalcone that binds strongly to MDM2 and irreversibly disrupts MDM2/p53 protein complex. Exhibits selective toxicity towards MDM2 overexpressing human breast cancer cell lines (IC50 = 10, 8.8, and 7 µM for MDA-MB-435, MDA-MB-231, and Wt-MCF7, respectively) compared to normal breast cell lines (IC50 = 75 and 63 µM for MCF-10A and MCF-12A, respectively).

Other Notes

Kumar, S.K., et al. 2003. J. Med. Chem.46, 2813.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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Srinivas K Kumar et al.
Journal of medicinal chemistry, 46(14), 2813-2815 (2003-06-27)
A series of boronic-chalcone derivatives were synthesized and tested for antitumor activity against human breast cancer cell lines. The results show the boronic-chalcones are more toxic to breast cancer cells compared to normal breast cells than other known chalcones.

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