1. Apoptosis
  2. IAP MDM-2/p53
  3. MDM2/XIAP-IN-1

MDM2/XIAP-IN-1 (compound 14) is an orally active inhibitor of dual MDM2/XIAP. MDM2/XIAP-IN-1 has anti-cancer activity with an IC50 value of 0.3 μM, which can be used in cance rescrch.

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MDM2/XIAP-IN-1

MDM2/XIAP-IN-1 Chemical Structure

CAS No. : 359595-95-2

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Description

MDM2/XIAP-IN-1 (compound 14) is an orally active inhibitor of dual MDM2/XIAP. MDM2/XIAP-IN-1 has anti-cancer activity with an IC50 value of 0.3 μM, which can be used in cance rescrch[1].

IC50 & Target

IC50:0.3 μM (EU-1 cell)[1]

In Vitro

MDM2/XIAP-IN-1 (0-4 μM, 48 h) inhibts the cell viability on two ALL cell lines (EU-1 and EU-3) and three NB cell lines (NB-1643, SHEP1, and LA1-55N)[1].
MDM2/XIAP-IN-1 degrades MDM2 and XIAP, killing tumor cells targeting, but not toxic to normal cells[1].

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

Clonogenic Assay:

Cell Line: NB and normal human hematopoietic cells[1]
Concentration: 0-4 μM
Incubation Time: 2 weeks
Result: Inhibited tumor cell growth, non-toxic to normal human hematopoietic cells.

Western Blot Analysis

Cell Line: EU-1 cell[1]
Concentration: 0-2 μM
Incubation Time: 0-24 h
Result: Caused the MDM2 and XIAP degradation as well as inducted p53 expression.
In Vivo

MDM2/XIAP-IN-1 Pharmacokinetic Analysis in Male SD rats Model[1]

Route Dose (mg/kg) AUClast (ng·h/mL) t1/2 (h) Clobs (L·h/kg) F (%)
i.v. 10 4750 0.94 2.12 /
p.o. 25 0.71 / / 5.9%

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

Masse moléculaire

488.60

Formule

C28H28N2O4S

CAS No.
SMILES

O=C(OC)C1=CC=C(C2NC3=C(C=C(S(=O)(NC4=CC=C(C)C(C)=C4)=O)C=C3)C5C2CC=C5)C=C1

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Pureté et documentation
Références
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Nom du produit:
MDM2/XIAP-IN-1
Cat. No.:
HY-153199
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