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MedKoo Cat#: 462282 | Name: DYRKs-IN-1

Description:

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

DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor and has antitumor activity.

Chemical Structure

DYRKs-IN-1
DYRKs-IN-1
CAS#1387090-01-8

Theoretical Analysis

MedKoo Cat#: 462282

Name: DYRKs-IN-1

CAS#: 1387090-01-8

Chemical Formula: C30H30ClN7O4

Exact Mass: 587.2048

Molecular Weight: 588.07

Elemental Analysis: C, 61.27; H, 5.14; Cl, 6.03; N, 16.67; O, 10.88

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.
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Related CAS #
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Synonym
DYRKs-IN-1
IUPAC/Chemical Name
N-(5-((3-amino-1-phenylpropyl)carbamoyl)-2-chlorophenyl)-2-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide
InChi Key
MRWURALZVKJHPD-UHFFFAOYSA-N
InChi Code
InChI=1S/C30H30ClN7O4/c31-23-9-6-18(27(39)34-24(10-11-32)17-4-2-1-3-5-17)13-25(23)35-28(40)22-12-19-14-33-30(37-26(19)36-29(22)41)38-15-20-7-8-21(16-38)42-20/h1-6,9,12-14,20-21,24H,7-8,10-11,15-16,32H2,(H,34,39)(H,35,40)(H,33,36,37,41)
SMILES Code
O=C(C1=CC2=CN=C(N3CC(O4)CCC4C3)N=C2NC1=O)NC5=CC(C(NC(C6=CC=CC=C6)CCN)=O)=CC=C5Cl
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
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively.
In vitro activity:
From a data-mining effort, the team has discovered analogues of pyrido[2,3-d]pyrimidines as potent enantio-selective inhibitors of DYRK1B. Cells treated with a tool compound from this series showed the same cellular effects as down regulation of DYRK1B with siRNA. Reference: Bioorg Med Chem Lett. 2013 Dec 15;23(24):6610-5. https://pubmed.ncbi.nlm.nih.gov/24239188/
In vivo activity:
TBD

Preparing Stock Solutions

The following data is based on the product molecular weight 588.07 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
Formulation protocol:
1. Anderson K, Chen Y, Chen Z, Dominique R, Glenn K, He Y, Janson C, Luk KC, Lukacs C, Polonskaia A, Qiao Q, Railkar A, Rossman P, Sun H, Xiang Q, Vilenchik M, Wovkulich P, Zhang X. Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6610-5. doi: 10.1016/j.bmcl.2013.10.055. Epub 2013 Nov 1. PMID: 24239188.
In vitro protocol:
1. Anderson K, Chen Y, Chen Z, Dominique R, Glenn K, He Y, Janson C, Luk KC, Lukacs C, Polonskaia A, Qiao Q, Railkar A, Rossman P, Sun H, Xiang Q, Vilenchik M, Wovkulich P, Zhang X. Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6610-5. doi: 10.1016/j.bmcl.2013.10.055. Epub 2013 Nov 1. PMID: 24239188.
In vivo protocol:
TBD
1: Kevin Anderson, et al. Pyrido pyrimidines. US20120184542A1 2: Anderson K, Chen Y, Chen Z, et al. Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors. Bioorg Med Chem Lett. 2013;23(24):6610-6615. doi:10.1016/j.bmcl.2013.10.055