Home Apoptosis MDM2/MDMX inhibitor SP141 For research use only.

SP141

SP141 is a new class of MDM2 inhibitor that promotes MDM2 auto-ubiquitination and degradation, and reduces levels of MDM2 in pancreatic cancer cell lines, as well as their proliferation and ability to form tumors in nude mice. SP141 inhibits human pancreatic cancer cell growth with IC50 values of less than 0.5 μM (0.38–0.50 μM) in a p53-independent manner.

SP141 Chemical Structure

SP141 Chemical Structure

CAS: 1253491-42-7

Purity & Quality Control

Batch: S090101 DMSO] 65 mg/mL] false] Ethanol] 65 mg/mL] false] Water] Insoluble] false Purity: 99.65%
99.65

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Biological Activity

Description SP141 is a new class of MDM2 inhibitor that promotes MDM2 auto-ubiquitination and degradation, and reduces levels of MDM2 in pancreatic cancer cell lines, as well as their proliferation and ability to form tumors in nude mice. SP141 inhibits human pancreatic cancer cell growth with IC50 values of less than 0.5 μM (0.38–0.50 μM) in a p53-independent manner.
Targets
MDM2 [1]
<0.50 μM
In vitro
In vitro

SP141 can bound directly to MDM2, promoting its auto-ubiquitination and degradation by the proteasome. SP141 reduces levels of MDM2 in pancreatic cancer cell lines, as well as their proliferation, with 50% inhibitory concentrations <0.5 μM (0.38–0.50 μM). Increasing concentrations of SP141 induces increasing levels of apoptosis and G2–M phase arrest of pancreatic cancer cell lines, whether or not they expressed functional P53.[1]
Cell Research Cell lines Humen pancreatic cancer cell lines
Concentrations 0.01-10 μM
Incubation Time 72 h
Method

Human pancreatic cancer cell lines (HPAC, Panc-1, AsPC-1, and Mia-Paca-2) are treated with various concentrations of SP141 or vehicle controls. And then cells are used to determine the effects of SP141 on the cell viability (MTT assay), colony formation,39 proliferation (BrdUrd incorporation assay), apoptosis, and cell cycle distribution.
In Vivo
In vivo

SP-141 (40 mg/kg; administered by i.p. injection; 5 d/wk for about three weeks) suppresses pancreatic tumor growth in both xenograft and orthotopic mouse models.[1]
Animal Research Animal Models Nude mice bearing Panc-1 xenograft tumors
Dosages 40 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 324.38 Formula

C22H16N2O
CAS No. 1253491-42-7 SDF --
Smiles COC1=CC2=C(C=C1)NC3=C2C=CN=C3C4=CC=CC5=CC=CC=C54
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 65 mg/mL ( (200.38 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 65 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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