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WM-S1-030

Chemical Structure : WM-S1-030

CAS No.: 2377507-01-0

WM-S1-030

Catalog No.: PC-21442Not For Human Use, Lab Use Only.

WM-S1-030 is a highly potent, specific inhibitor of recepteur d'origine nantais (RON kinase, MST1R) with IC50 of 0.39 nM in in vitro enzyme activity.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

WM-S1-030 is a highly potent, specific inhibitor of recepteur d'origine nantais (RON kinase, MST1R) with IC50 of 0.39 nM in in vitro enzyme activity.
WM-S1-030 inhibits the activity of Met family members and a few tyrosine kinases (TKs) (Axl, Flt4, Mer, and TRKC), with IC50 values < 10 nM.
WM-S1-030 is >100-fold selective for the TKs DDR2, Flt3, IGF1R, and ROS, and >1000-fold selective for all other kinases against a panel of kinases, except Fms, KDR and TrkA.
WM-S1-030 shows strong potency against colo320HSR cells, with IC50 values of 27.41 nM, 98.7 nM, and 137.2 nM, in cell lines expressing RONΔ160, RONΔ155, and RONΔ165, respectively, which is much more potent than BMS777607.
WM-S1-030 effectively inhibits the RON variants and exerts potent anticancer efficacy in RON variant-positive colon cancer.
WM-S1-030 elicits notable antitumor immunity in anti-PD-1 resistant cell derived mouse model.

Physicochemical Properties

M.Wt 695.74
Formula C37H31F2N5O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-ethoxy-N-(3-fluoro-4-((2-(5-(morpholinomethyl)pyridin-2-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide

References

1. Joseph Kim, et al. Cell Death Differ. 2023 Nov 6. doi: 10.1038/s41418-023-01235-9.

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