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Chemical Structure| 1247927-81-6 Chemical Structure| 1247927-81-6

Structure of 1247927-81-6

Chemical Structure| 1247927-81-6

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Product Citations

Product Citations

Li, Kaixuan ; Wang, Mingqian ; Akoglu, Melike ; Pollard, Alyssa C. ; Klecker, John B. ; Alfonso, Patricia , et al.

Abstract: Bruton′s tyrosine kinase (BTK) is a target for treating B-cell malignancies and autoimmune diseases. To aid in the discovery and development of BTK inhibitors and improve clin. diagnoses, we have developed a positron emission tomog. (PET) radiotracer based on a selective BTK inhibitor, remibrutinib. [18F]PTBTK3 is an aromatic, 18F-labeled tracer that was synthesized in 3 steps with a 14.8 ± 2.4% decay-corrected radiochem. yield and ≥99% radiochem. purity. The cellular uptake of [18F]PTBTK3 was blocked up to 97% in JeKo-1 cells using remibrutinib or non-radioactive PTBTK3. [18F]PTBTK3 exhibited renal and hepatobiliary clearance in NOD SCID (non-obese diabetic/ severe combined immunodeficiency) mice, and the tumor uptake of [18F]PTBTK3 in BTK-pos. JeKo-1 xenografts (1.23 ± 0.30% ID/cc) was significantly greater at 60 min post injection compared to the tumor uptake in BTK-neg. U87MG xenografts (0.41 ± 0.11% ID/cc). In the JeKo-1 xenografts, tumor uptake was blocked up to 62% by remibrutinib, indicating the BTK-dependent uptake of [18F]PTBTK3 in tumors.

Keywords: PET imaging ; BTK ; tumor ; fluorine-18 ; Jeko-1 ; U87MG

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Product Details of [ 1247927-81-6 ]

CAS No. :1247927-81-6
Formula : C10H9FO2
M.W : 180.18
SMILES Code : O=C(O)C1=CC=C(C2CC2)C=C1F
MDL No. :MFCD16778841
Boiling Point : No data available

Safety of [ 1247927-81-6 ]

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P362-P403+P233-P501
 

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