[ CAS No. 29022-11-5 ] {[proInfo.proName]}

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Quality Control of [ 29022-11-5 ]

COA NMR CNMR HPLC LC-MS

Related Doc. of [ 29022-11-5 ]

SDS Specification

Alternatived Products of [ 29022-11-5 ]

Product Citations

Shorter Peptide Nucleic Acid Probes Improve Affibody-Mediated Peptide Nucleic Acid-Based Pretargeting

Kristina Westerlund ; Maryam Oroujeni ; Maxime Gestin , et al. ACS Pharmacol. Transl. Sci.,2024,7(5):1595-1611. DOI: 10.1021/acsptsci.4c00106

Abstract: Affibody-mediated PNA-based pretargeting shows promise for HER2-expressing tumor radiotherapy. In our recent study, a 15-mer ZHER2:342-HP15 affibody-PNA conjugate, in combination with a shorter 9-mer [177Lu]Lu-HP16 effector probe, emerged as the most effective pretargeting strategy. It offered a superior tumor-to-kidney uptake ratio and more efficient tumor targeting compared to longer radiolabeled effector probes containing 12 or 15 complementary PNA bases. To enhance the production efficiency of our pretargeting system, we here introduce even shorter 6-, 7-, and 8-mer secondary probes, designated as HP19, HP21, and HP20, respectively. We also explore the replacement of the original 15-mer Z-HP15 primary probe with shorter 12-mer Z-HP12 and 9-mer Z-HP9 alternatives. This extended panel of shorter PNA-based probes was synthesized using automated microwave-assisted methods and biophysically screened in vitro to identify shorter probe combinations with the most effective binding properties. In a mouse xenograft model, we evaluated the biodistribution of these probes, comparing them to the Z-HP15:[177Lu]Lu-HP16 combination. Tumor-to-kidney ratios at 4 and 144 h postinjection of the secondary probe showed no significant differences among the Z-HP9:[177Lu]Lu-HP16, Z-HP9:[177Lu]Lu-HP20, and the Z-HP15:[177Lu]Lu-HP16 pairs. Importantly, tumor uptake significantly exceeded, by several hundred-fold, that of most normal tissues, with kidney uptake being the critical organ for radiation therapy. This suggests that using a shorter 9-mer primary probe, Z-HP9, in combination with 9-mer HP16 or 8-mer HP20 secondary probes effectively targets tumors while minimizing the dose-limiting kidney uptake of radionuclide. In conclusion, the Z-HP9:HP16 and Z-HP9:HP20 probe combinations offer good prospects for both cost-effective production and efficient in vivo pretargeting of HER2-expressing tumors.

Keywords: affibody ; pretargeting ; peptide nucleic acid ; radiotherapy

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Product Details of [ 29022-11-5 ]

CAS No. :	29022-11-5	MDL No. :	MFCD00037140
Formula :	C₁₇H₁₅NO₄	Boiling Point :	-
Linear Structure Formula :	(C₁₅H₁₁O₂)NHCH₂COOH	InChI Key :	NDKDFTQNXLHCGO-UHFFFAOYSA-N
M.W :	297.31	Pubchem ID :	93124
Synonyms :	Fmoc glycine;N-(9-Fluorenylmethoxycarbonyl)glycine;[[[(9H-Fluoren-9-yl)methoxy]carbonyl]amino]acetic acid;NSC 334288;NPC 14692;N-Fluorenylmethoxycarbonylglycine	Chemical Name :	2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)acetic acid

Safety of [ 29022-11-5 ]

Signal Word:	Warning	Class:	N/A
Precautionary Statements:	P261-P305+P351+P338	UN#:	N/A
Hazard Statements:	H315-H319-H335	Packing Group:	N/A
GHS Pictogram:

Application In Synthesis of [ 29022-11-5 ]

* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.

Downstream synthetic route of [ 29022-11-5 ]

[ 29022-11-5 ] Synthesis Path-Downstream 1~7

1
[ 29022-11-5 ]
[ 71989-31-6 ]
[ 35661-40-6 ]
[ 108-24-7 ]
[ 198561-07-8 ]
Ac-Pro-Asp-Phe-Gly-OH [ No CAS ]