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MedKoo Cat#: 128021 | Name: DYR684

Description:

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

DYR684 is a Potent, Selective, and Metabolically Stable PROTAC of the Protein Kinases DYRK1A and DYRK1B. DYR684 promoted fast, efficient, potent, and selective degradation of DYRK1A in cellbased assays. Interestingly, an enzymatically inactive splicing variant of DYRK1B (p65) resisted degradation. Compared to competitive kinase inhibition, targeted degradation of DYRK1 by DYR684 provided improved suppression of downstream signaling.

Chemical Structure

DYR684

CAS#N/A

Theoretical Analysis

MedKoo Cat#: 128021

Name: DYR684

CAS#: N/A

Chemical Formula: C58H58FN15O5

Exact Mass: 1063.4729

Molecular Weight: 1064.20

Elemental Analysis: C, 65.46; H, 5.49; F, 1.79; N, 19.74; O, 7.52

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

DYR684; DYR 684; DYR-684

IUPAC/Chemical Name

4-(((1-(1-(1-(5-(3-(4-(4-(5-(2-aminopyridin-4-yl)-2-methyl-3H-imidazo[4,5-b]pyridin-3-yl)-2-fluorophenyl)piperazin-1-yl)prop-1-yn-1-yl)pyridin-2-yl)piperidine-4-carbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)methyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

InChi Key

PTARASCXNREVCH-UHFFFAOYSA-N

InChi Code

InChI=1S/C58H58FN15O5/c1-36-65-47-10-9-45(40-15-20-61-50(60)30-40)66-54(47)73(36)42-8-11-48(44(59)31-42)69-28-26-68(27-29-69)21-3-4-37-7-13-51(63-32-37)70-22-16-39(17-23-70)56(77)71-24-18-41(19-25-71)72-35-38(34-64-72)33-62-46-6-2-5-43-53(46)58(79)74(57(43)78)49-12-14-52(75)67-55(49)76/h2,5-11,13,15,20,30-32,34-35,39,41,49,62H,12,14,16-19,21-29,33H2,1H3,(H2,60,61)(H,67,75,76)

SMILES Code

NC1=NC=CC(C2=NC(N(C3=CC(F)=C(N4CCN(CC#CC5=CN=C(N6CCC(C(N7CCC(N8N=CC(CNC9=C(C(N(C%10CCC(NC%10=O)=O)C%11=O)=O)C%11=CC=C9)=C8)CC7)=O)CC6)C=C5)CC4)C=C3)C(C)=N%12)=C%12C=C2)=C1

Appearance

To be determined

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 1,064.20 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.

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

Wilms G, Schofield K, Maddern S, Foley C, Shaw Y, Smith B, Basantes LE, Schwandt K, Babendreyer A, Chavez T, McKee N, Gokhale V, Kallabis S, Meissner F, Rokey SN, Dunckley T, Montfort WR, Becker W, Hulme C. Discovery and Functional Characterization of a Potent, Selective, and Metabolically Stable PROTAC of the Protein Kinases DYRK1A and DYRK1B. J Med Chem. 2024 Oct 10;67(19):17259-17289. doi: 10.1021/acs.jmedchem.4c01130. Epub 2024 Sep 30. PMID: 39344427.