Home Apoptosis MDM2/MDMX inhibitor SP141

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SP141 MDM2/MDMX inhibitor

Cat.No.S0901

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. This compound 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 MDM2/MDMX inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 324.38

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (200.38 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 65 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 324.38 Formula

C22H16N2O

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1253491-42-7 -- Storage of Stock Solutions

Synonyms N/A Smiles COC1=CC2=C(C=C1)NC3=C2C=CN=C3C4=CC=CC5=CC=CC=C54

Mechanism of Action

Targets/IC50/Ki
MDM2
<0.50 μM
In vitro

SP141 can bound directly to MDM2, promoting its auto-ubiquitination and degradation by the proteasome. This compound 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 this chemical induces increasing levels of apoptosis and G2–M phase arrest of pancreatic cancer cell lines, whether or not they expressed functional P53.
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.
References

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