MedKoo Cat#: 206544 | Name: BAY1143269
Featured

Description:

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

BAY1143269 is an orally bioavailable inhibitor of mitogen-activated protein kinase interacting serine/threonine-protein kinase 1 (MKNK1), with potential antineoplastic activity. Upon oral administration, MKNK1 inhibitor BAY 1143269 binds to MKNK1, thereby preventing its activation and the downstream MKNK1-mediated phosphorylation and activation of eukaryotic translation initiation factor 4E (eIF4E). As eIF4E enhances the synthesis of oncogenic proteins, preventing eIF4E activity inhibits the synthesis of tumor angiogenic factors and leads to both the inhibition of cellular proliferation and apoptosis in susceptible tumor cells.

Chemical Structure

BAY1143269
BAY1143269
CAS#1426928-20-2

Theoretical Analysis

MedKoo Cat#: 206544

Name: BAY1143269

CAS#: 1426928-20-2

Chemical Formula: C17H16N4O2

Exact Mass: 308.1273

Molecular Weight: 308.34

Elemental Analysis: C, 66.22; H, 5.23; N, 18.17; O, 10.38

Price and Availability

Size Price Availability Quantity
5mg USD 450.00 2 Weeks
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
No Data
Synonym
BAY1143269; BAY 1143269; BAY-1143269.
IUPAC/Chemical Name
(R)-2-((3-(benzofuran-2-yl)imidazo[1,2-b]pyridazin-6-yl)oxy)propan-1-amine
InChi Key
CMDIADSAZCFCCT-LLVKDONJSA-N
InChi Code
InChI=1S/C17H16N4O2/c1-11(9-18)22-17-7-6-16-19-10-13(21(16)20-17)15-8-12-4-2-3-5-14(12)23-15/h2-8,10-11H,9,18H2,1H3/t11-/m1/s1
SMILES Code
NC[C@@H](C)OC1=NN2C(C3=CC4=CC=CC=C4O3)=CN=C2C=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
Soluble in DMSO, not in water
Shelf Life
>2 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
BAY1143269 acted on GMECs by suppressing the eukaryotic translation initiation factor 4E (eIF4E) and eIF4E-mediated expression of oncogenic proteins, including those involved in cell cycle, epithelial-mesenchymal transition (EMT), and pro-survival. In addition, BAY1143269 suppressed eIF4E phosphorylation, inhibited proliferation, and induced apoptosis of glioblastoma cells. Interestingly, it reduced vascular endothelial growth factor (VEGF) level in tumor cells and culturing medium, demonstrating the inhibitory effect of BAY1143269 on tumor proangiogenic microenvironment. We finally challenged BAY1143269 on the glioblastoma xenograft mice model and observed a significant tumor growth reduction without toxicity in mice receiving oral BAY1143269. Immunoblotting analysis demonstrated significantly less phosphorylated-eIF4E (p-eIF4E), cluster of differentiation 31 (CD31) (microvascular endothelial cell marker), and VEGF in tumors from drug-treated mice. In summary, the inhibition of glioblastoma angiogenesis with BAY1143269 may provide an alternative approach for anti-glioblastoma therapy.

Preparing Stock Solutions

The following data is based on the product molecular weight 308.34 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: Jin X, Yu R, Wang X, Proud CG, Jiang T. Progress in developing MNK inhibitors. Eur J Med Chem. 2021 Jul 5;219:113420. doi: 10.1016/j.ejmech.2021.113420. Epub 2021 Apr 2. PMID: 33892273. 2: Wan W, Zhang X, Huang C, Chen L, Yang X, Bao K, Peng T. Preclinical anti- angiogenic and anti-cancer activities of BAY1143269 in glioblastoma via targeting oncogenic protein expression. Pharmacol Res Perspect. 2022 Aug;10(4):e00981. doi: 10.1002/prp2.981. PMID: 35796398; PMCID: PMC9260954.