5.32814
MDM2 Inhibitor, SP-141
Synonym(s):
MDM2 Inhibitor, SP-141, SP141, SP 141
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About This Item
Empirical Formula (Hill Notation):
C22H16N2O
CAS Number:
Molecular Weight:
324.38
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥97% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
assay
≥97% (HPLC)
Quality Segment
form
powder
potency
28 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
SMILES string
COC1=CC=C(NC2=C3C=CN=C2C4=CC=CC5=C4C=CC=C5)C3=C1
InChI
1S/C22H16N2O/c1-25-15-9-10-20-19(13-15)18-11-12-23-21(22(18)24-20)17-8-4-6-14-5-2-3-7-16(14)17/h2-13,24H,1H3
InChI key
AABFWJDLCCDJJN-UHFFFAOYSA-N
General description
A cell-permeable compound that binds to MDM2 with high affinity (Ki = 28 nM) and inhibits its activity in multiple breast cancer cell lines, independent of their p53 status.
A cell-permeable pyrido[3,4-b]indole derivative that binds directly to the hydrophobic groove of MDM2 with high affinity (Ki = 28 nM) and inhibits its activity in multiple breast cancer cell lines, independent of their p53 status. Exhibits higher binding affinity than nutlin-3 (Kd = 45 nM). Acts by reducing MDM2 expression and promoting its ubiquitination and proteasomal degradation. Induces cell cycle arrest at the G2 phase and induces apoptosis in MCF-7, MCF-7 KD, and MDA-MB-468 breast cancer cells in a concentration-dependent manner. Also reported to diminish cell migration and reduce metastasis of breast cancer cells. Suppresses the growth of MCF-7 and MDA-MB-468 xenografts in nude mice (40 mg/kg/ 30 or 42 days, i.p.).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MDM2
MDM2
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Wang, W., et al. 2014. Nat. Comm.5, 5086.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
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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