PSA is one of the most studied biomarkers for Prostate Cancer. However, serum PSA levels are mildly elevated in both malignant and non-malignant prostate conditions. Enzymatically active PSA, present at detectable levels only in prostate tumor tissue, provides a better target to measure the malignancy of prostate cancer.

PSA 750 FAST™ is a unique type of activatable in vivo fluorescent agent that detects and quantifies PSA enzymatic activity at sites of prostate tumor growth.

• Detect and quantify active PSA non-invasively in vivo

• Selective against unbound and complexed PSA

• High Specificity for PSA+ tumors

• Validated on PerkinElmer’s comprehensive line of in vivo imaging systems

PSA 750 FASTActivatable Fluorescent Pre-clinical Imaging Agent

QUANTIFY ACTIVE PSAIN VIVO

PSA 750 FAST™ Mechanism of Action

PSA 750 FAST™ has been validated on both the IVIS and the FMT platforms. Images above show clear targeting to PSA+ LNCaP tumors. Mice were injected with 2 nmoles of PSA agent and imaged 24 hours post injection.

IVIS Spectrum FMT 2D FMT 3D

Quenched

Fluorescent Fluorescent

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010476_01 Printed in USA August 2012

PerkinElmer, Inc. 940 Winter Street Waltham, MA 02451 USA P: (800) 762-4000 or (+1) 203-925-4602www.perkinelmer.com

(A) - In vivo imaging in PSA+ and PSA- tumors after injection of PSA 750 FAST™. Tumor-bearing male Nu/Nu injected i.v. with 2 nmoles of agent and imaged 24 hours later. Four mice were implanted with either LNCaP (PSA+) or PC-3 (PSA-) cells. Images show concentration of the agent (pmoles) in tumor bearing mice. (B) - Chart on the top shows tumor fluorescence significantly higher in PSA+ LNCaP than in PSA- PC-3 tumors in vivo. Bottom graph shows a very good correlation between tumor signal and tumor size (C) - Enzyme biochemistry validation showing PSA 750 FAST™ is specifically cleaved by active PSA over inactive PSA (complexed with its inhibitor a1-antichymotrypsin), and other disease-relevant enzymes. (D) - Ex vivo validation of the specificity of PSA 750 FAST™ by microscopy. Complete blockage of fluorescent signal observed after pre-incubating tumor sections with the PSA natural inhibitor, a1-antichymotrypsin.

A

C

B

D

PSA+ LNCaP

5.5 pmol

16.8 pmol

58.9 pmol1.9 pmol

31.2 pmol

5.8 pmol6.6 pmol

2.7 pmol

PSA- PC-3

Learn more at www.perkinelmer.com/invivoreagents

PerkinElmer in vivo imaging reagents are intended for animal research and not for use in humans.

Validated and optimized for use on all PerkinElmer's in vivo imaging systems

IVIS® Spectrum CT FMT® 4000 Maestro™ 2 Quantum FX μCT