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MTX-216

Chemical Structure : MTX-216

CAS No.: 1952236-19-9

MTX-216 (MTX216)

Catalog No.: PC-49627Not For Human Use, Lab Use Only.

MTX-216 (MTX216) is a dual PI3K/EGFR inhibitor that blocks neurofibromin 1 loss of function (NF1LoF) melanoma cell growth in vitro and in vivo, suppresses the activity of SYK kinase with IC50 of 281 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

MTX-216 (MTX216) is a dual PI3K/EGFR inhibitor that blocks neurofibromin 1 loss of function (NF1LoF) melanoma cell growth in vitro and in vivo, suppresses the activity of SYK kinase with IC50 of 281 nM.
MTX-216 at 1 μmol/L inhibited p-SYK expression in MeWo cells by approximately 50%, reduced p-BLNK levels in IgM-stimulated Ramos cells.
MTX-216 increases NF1LoF melanoma cells sensitivity to both PI3K and MEK inhibitors, suppresses genes that regulate mitochondrial ETC in NF1LoF cells.
MTX-216 effectively suppressed both Ki-67 and p-S6 in NF1LoF melanoma cells, inducing efficacious antitumor responses in these cells.

Physicochemical Properties

M.Wt 502.35
Formula C22H14Cl2FN5O2S
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

N-(2-chloro-5-(4-((3-chloro-4-fluorophenyl)amino)-3-cyanoquinolin-6-yl)pyridin-3-yl)methanesulfonamide

References

1. Cara Abecunas, et al. Cancer Res. 2023 Jan 18;83(2):316-331.

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