MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 465457 | Name: PI-2620

Description:

WARNING: This product is for research use only, not for human or veterinary use.

PI-2620 is a useful agent for the Detection of Pathological Aggregated Tau in Alzheimer’s Disease and Other Tauopathies. PI-2620 emerged as a best candidate displaying high Tau binding, low MAO-A binding, high brain uptake, and fast and complete brain washout. Furthermore, PI-2620 showed Tau binding on brain sections from corticobasal degeneration, progressive supranuclear palsy, and Pick’s disease.

Chemical Structure

PI-2620
PI-2620
CAS#unknown

Theoretical Analysis

MedKoo Cat#: 465457

Name: PI-2620

CAS#: unknown

Chemical Formula: C15H9FN4

Exact Mass: 264.0811

Molecular Weight: 264.26

Elemental Analysis: C, 68.18; H, 3.43; F, 7.19; N, 21.20

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
Bulk Inquiry
Related CAS #
No Data
Synonym
PI-2620; PI2620; PI 2620;
IUPAC/Chemical Name
2-(2-fluoropyridin-4-yl)-9H-pyrrolo[2,3-b:4,5-c']dipyridine
InChi Key
JUPWIBZGGFVBCU-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H9FN4/c16-14-7-9(3-6-18-14)12-2-1-10-11-8-17-5-4-13(11)20-15(10)19-12/h1-8H,(H,19,20)
SMILES Code
FC1=NC=CC(C2=CC=C3C(NC4=C3C=NC=C4)=N2)=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 264.26 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Kroth H, Oden F, Molette J, Schieferstein H, Gabellieri E, Mueller A, Berndt M, Sreenivasachary N, Serra AM, Capotosti F, Schmitt-Willich H, Hickman D, Pfeifer A, Dinkelborg L, Stephens A. PI-2620 Lead Optimization Highlights the Importance of Off-Target Assays to Develop a PET Tracer for the Detection of Pathological Aggregated Tau in Alzheimer's Disease and Other Tauopathies. J Med Chem. 2021 Aug 29. doi: 10.1021/acs.jmedchem.1c00861. Epub ahead of print. PMID: 34455780. 2: Jantarato A, Vachatimanont S, Boonkawin N, Yaset S, Kunawudhi A, Promteangtrong C, Assanasen J, Mahanonda N, Chotipanich C. The Evaluation of Tau Deposition with [18F]PI-2620 by Using a Semiquantitative Method in Cognitively Normal Subjects and Patients with Mild Cognitive Impairment and Alzheimer's Disease. Mol Imaging. 2021 Jul 9;2021:6640054. doi: 10.1155/2021/6640054. PMID: 34381315; PMCID: PMC8328488. 3: Carlson ML, Toueg TN, Khalighi MM, Castillo J, Shen B, Azevedo EC, DiGiacomo P, Mouchawar N, Chau G, Zaharchuk G, James ML, Mormino EC, Zeineh MM. Hippocampal subfield imaging and fractional anisotropy show parallel changes in Alzheimer's disease tau progression using simultaneous tau-PET/MRI at 3T. Alzheimers Dement (Amst). 2021 Jul 28;13(1):e12218. doi: 10.1002/dad2.12218. PMID: 34337132; PMCID: PMC8319659. 4: Willroider M, Roeber S, Horn AKE, Arzberger T, Scheifele M, Respondek G, Sabri O, Barthel H, Patt M, Mishchenko O, Schildan A, Mueller A, Koglin N, Stephens A, Levin J, Höglinger GU, Bartenstein P, Herms J, Brendel M, Beyer L. Superiority of Formalin-Fixed Paraffin-Embedded Brain Tissue for in vitro Assessment of Progressive Supranuclear Palsy Tau Pathology With [ 18 F]PI-2620. Front Neurol. 2021 Jul 2;12:684523. doi: 10.3389/fneur.2021.684523. PMID: 34276540; PMCID: PMC8282895. 5: Kim HJ, Jo S, Lee S, Oh M, Lee JH. Crossed Hemispheric Accumulation of β-Amyloid and Tau Protein in a Patient With Typical Alzheimer Disease. Alzheimer Dis Assoc Disord. 2021 Jun 16. doi: 10.1097/WAD.0000000000000460. Epub ahead of print. PMID: 34132670. 6: Song M, Beyer L, Kaiser L, Barthel H, van Eimeren T, Marek K, Nitschmann A, Scheifele M, Palleis C, Respondek G, Kern M, Biechele G, Hammes J, Bischof G, Barbe M, Onur Ö, Jessen F, Saur D, Schroeter ML, Rumpf JJ, Rullmann M, Schildan A, Patt M, Neumaier B, Barret O, Madonia J, Russell DS, Stephens AW, Mueller A, Roeber S, Herms J, Bötzel K, Danek A, Levin J, Classen J, Höglinger GU, Bartenstein P, Villemagne V, Drzezga A, Seibyl J, Sabri O, Boening G, Ziegler S, Brendel M. Binding characteristics of [18F]PI-2620 distinguish the clinically predicted tau isoform in different tauopathies by PET. J Cereb Blood Flow Metab. 2021 May 27:271678X211018904. doi: 10.1177/0271678X211018904. Epub ahead of print. PMID: 34044665. 7: Song M, Scheifele M, Barthel H, van Eimeren T, Beyer L, Marek K, Eckenweber F, Palleis C, Kaiser L, Finze A, Kern M, Nitschmann A, Biechele G, Katzdobler S, Bischof G, Hammes J, Jessen F, Saur D, Schroeter ML, Rumpf JJ, Rullmann M, Schildan A, Patt M, Neumaier B, Stephens AW, Rauchmann BS, Perneczky R, Levin J, Classen J, Höglinger GU, Bartenstein P, Boening G, Ziegler S, Villemagne V, Drzezga A, Seibyl J, Sabri O, Brendel M; German Imaging Initiative for Tauopathies (GII4T). Feasibility of short imaging protocols for [18F]PI-2620 tau-PET in progressive supranuclear palsy. Eur J Nucl Med Mol Imaging. 2021 May 22. doi: 10.1007/s00259-021-05391-3. Epub ahead of print. PMID: 34021393. 8: Palleis C, Brendel M, Finze A, Weidinger E, Bötzel K, Danek A, Beyer L, Nitschmann A, Kern M, Biechele G, Rauchmann BS, Häckert J, Höllerhage M, Stephens AW, Drzezga A, van Eimeren T, Villemagne VL, Schildan A, Barthel H, Patt M, Sabri O; German Imaging Initiative for Tauopathies (GII4T), Bartenstein P, Perneczky R, Haass C, Levin J, Höglinger GU. Cortical [18 F]PI-2620 Binding Differentiates Corticobasal Syndrome Subtypes. Mov Disord. 2021 May 5. doi: 10.1002/mds.28624. Epub ahead of print. PMID: 33951244. 9: Aghakhanyan G, Saur D, Rullmann M, Weise CM, Schroeter ML, Marek K, Jamra RA, Tiepolt S, Strauss M, Scherlach C, Hoffmann KT, Sabri O, Classen J, Barthel H. PET/MRI Delivers Multimodal Brain Signature in Alzheimer's Disease with De Novo PSEN1 Mutation. Curr Alzheimer Res. 2021;18(2):178-184. doi: 10.2174/1567205018666210414111536. PMID: 33855944. 10: Nuebling GS, Prix C, Brendel M, Beyer L, Wlasich E, Loosli SV, Barthel H, Sabri O, Bartenstein P, Vöglein J, Danek A, Rominger A, Edbauer D, Haass C, Levin J. Low-degree trisomy 21 mosaicism promotes early-onset Alzheimer disease. Neurobiol Aging. 2021 Jul;103:147.e1-147.e5. doi: 10.1016/j.neurobiolaging.2021.02.021. Epub 2021 Feb 28. PMID: 33789815. 11: Beyer L, Brendel M. Imaging of Tau Pathology in Neurodegenerative Diseases: An Update. Semin Nucl Med. 2021 May;51(3):253-263. doi: 10.1053/j.semnuclmed.2020.12.004. Epub 2020 Dec 20. PMID: 33353724. 12: Brendel M, Barthel H, van Eimeren T, Marek K, Beyer L, Song M, Palleis C, Gehmeyr M, Fietzek U, Respondek G, Sauerbeck J, Nitschmann A, Zach C, Hammes J, Barbe MT, Onur O, Jessen F, Saur D, Schroeter ML, Rumpf JJ, Rullmann M, Schildan A, Patt M, Neumaier B, Barret O, Madonia J, Russell DS, Stephens A, Roeber S, Herms J, Bötzel K, Classen J, Bartenstein P, Villemagne V, Levin J, Höglinger GU, Drzezga A, Seibyl J, Sabri O. Assessment of 18F-PI-2620 as a Biomarker in Progressive Supranuclear Palsy. JAMA Neurol. 2020 Nov 1;77(11):1408-1419. doi: 10.1001/jamaneurol.2020.2526. Erratum in: JAMA Neurol. 2020 Nov 1;77(11):1453. PMID: 33165511; PMCID: PMC7341407. 13: Oh M, Oh SJ, Lee SJ, Oh JS, Roh JH, Chung SJ, Lee JH, Lee CS, Kim JS. Clinical Evaluation of 18F-PI-2620 as a Potent PET Radiotracer Imaging Tau Protein in Alzheimer Disease and Other Neurodegenerative Diseases Compared With 18F-THK-5351. Clin Nucl Med. 2020 Nov;45(11):841-847. doi: 10.1097/RLU.0000000000003261. PMID: 32910050. 14: Chotipanich C, Nivorn M, Kunawudhi A, Promteangtrong C, Boonkawin N, Jantarato A. Evaluation of Imaging Windows for Tau PET Imaging Using 18F-PI2620 in Cognitively Normal Individuals, Mild Cognitive Impairment, and Alzheimer's Disease Patients. Mol Imaging. 2020 Jan- Dec;19:1536012120947582. doi: 10.1177/1536012120947582. PMID: 32862780; PMCID: PMC7466905. 15: Mormino EC, Toueg TN, Azevedo C, Castillo JB, Guo W, Nadiadwala A, Corso NK, Hall JN, Fan A, Trelle AN, Harrison MB, Hunt MP, Sha SJ, Deutsch G, James M, Fredericks CA, Koran ME, Zeineh M, Poston K, Greicius MD, Khalighi M, Davidzon GA, Shen B, Zaharchuk G, Wagner AD, Chin FT. Tau PET imaging with 18F-PI-2620 in aging and neurodegenerative diseases. Eur J Nucl Med Mol Imaging. 2021 Jul;48(7):2233-2244. doi: 10.1007/s00259-020-04923-7. Epub 2020 Jun 23. PMID: 32572562; PMCID: PMC7755737. 16: Beyer L, Nitschmann A, Barthel H, van Eimeren T, Unterrainer M, Sauerbeck J, Marek K, Song M, Palleis C, Respondek G, Hammes J, Barbe MT, Onur Ö, Jessen F, Saur D, Schroeter ML, Rumpf JJ, Rullmann M, Schildan A, Patt M, Neumaier B, Barret O, Madonia J, Russell DS, Stephens AW, Roeber S, Herms J, Bötzel K, Levin J, Classen J, Höglinger GU, Bartenstein P, Villemagne V, Drzezga A, Seibyl J, Sabri O, Brendel M. Early-phase [18F]PI-2620 tau-PET imaging as a surrogate marker of neuronal injury. Eur J Nucl Med Mol Imaging. 2020 Nov;47(12):2911-2922. doi: 10.1007/s00259-020-04788-w. Epub 2020 Apr 21. PMID: 32318783; PMCID: PMC7567714. 17: Bullich S, Barret O, Constantinescu C, Sandiego C, Mueller A, Berndt M, Papin C, Perrotin A, Koglin N, Kroth H, Pfeifer A, Tamagnan G, Madonia J, Seibyl JP, Marek K, De Santi S, Dinkelborg LM, Stephens AW. Evaluation of Dosimetry, Quantitative Methods, and Test-Retest Variability of 18F-PI-2620 PET for the Assessment of Tau Deposits in the Human Brain. J Nucl Med. 2020 Jun;61(6):920-927. doi: 10.2967/jnumed.119.236240. Epub 2019 Nov 11. PMID: 31712324; PMCID: PMC7262221. 18: Mueller A, Bullich S, Barret O, Madonia J, Berndt M, Papin C, Perrotin A, Koglin N, Kroth H, Pfeifer A, Tamagnan G, Seibyl JP, Marek K, De Santi S, Dinkelborg LM, Stephens AW. Tau PET imaging with 18F-PI-2620 in Patients with Alzheimer Disease and Healthy Controls: A First-in-Humans Study. J Nucl Med. 2020 Jun;61(6):911-919. doi: 10.2967/jnumed.119.236224. Epub 2019 Nov 11. PMID: 31712323; PMCID: PMC7262222. 19: Kroth H, Oden F, Molette J, Schieferstein H, Capotosti F, Mueller A, Berndt M, Schmitt-Willich H, Darmency V, Gabellieri E, Boudou C, Juergens T, Varisco Y, Vokali E, Hickman DT, Tamagnan G, Pfeifer A, Dinkelborg L, Muhs A, Stephens A. Discovery and preclinical characterization of [18F]PI-2620, a next- generation tau PET tracer for the assessment of tau pathology in Alzheimer's disease and other tauopathies. Eur J Nucl Med Mol Imaging. 2019 Sep;46(10):2178-2189. doi: 10.1007/s00259-019-04397-2. Epub 2019 Jul 1. PMID: 31264169; PMCID: PMC6667408. 20: Murugan NA, Chiotis K, Rodriguez-Vieitez E, Lemoine L, Ågren H, Nordberg A. Cross-interaction of tau PET tracers with monoamine oxidase B: evidence from in silico modelling and in vivo imaging. Eur J Nucl Med Mol Imaging. 2019 Jun;46(6):1369-1382. doi: 10.1007/s00259-019-04305-8. Epub 2019 Mar 27. PMID: 30919054; PMCID: PMC6486902.

View History

PiB

PiB