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Chemical Structure| 38953-42-3 Chemical Structure| 38953-42-3

Structure of 38953-42-3

Chemical Structure| 38953-42-3

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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 [ 38953-42-3 ]

CAS No. :38953-42-3
Formula : C4H4ClN3O
M.W : 145.55
SMILES Code : OC1=C(Cl)N=CN=C1N
MDL No. :MFCD13689013
InChI Key :PLOZXUFHBRJLFX-UHFFFAOYSA-N
Pubchem ID :13012885

Safety of [ 38953-42-3 ]

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P261-P280-P305+P351+P338
 

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Related Functional Groups of
[ 38953-42-3 ]

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Related Parent Nucleus of
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