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ARN22089

Chemical Structure : ARN22089

CAS No.: 2248691-29-2

ARN22089 (ARN 22089)

Catalog No.: PC-38415Not For Human Use, Lab Use Only.

ARN22089 (ARN 22089) is a specific small molecule inhibitor of putative CDC42 family effector interaction, binds to CDC42 and has broad anti-cancer activity and inhibits MAPK and S6 signaling.

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Biological Activity

ARN22089 (ARN 22089) is a specific small molecule inhibitor of putative CDC42 family effector interaction, binds to CDC42 and has broad anti-cancer activity and inhibits MAPK and S6 signaling.
ARN22089 could inhibit CDC42-PAK interactions with EC50 of 0.1 uM, and inhibit RHOJ/PAK interactions with approximate EC50 of 1-5 uM.
ARN22089 has a single-digit micromolar IC50 activity against sensitive cell lines (WM3248, SKMel3, A375, and SW480), has IC50 of < 10 uM for 55/100 cell lines in a panel of 100 cancer cell lines with various different mutations, including several cell lines with neuroblastoma RAS (NRAS) mutations.
ARN22089 inhibits MAPK and S6 phosphorylation and influences NFkB signaling in vitro.
ARN22089 specifically inhibits tumor angiogenesis in 3D vascularized microtumors, shows drug-like properties and inhibits tumor growth in vivo.
ARN22089 selectively binds and inhibits CDC42 effector interactions.
ARN22089 binds better to the purified CDC42 compared with other known CDC42 inhibitors (ZCL278, ML141, R-ketoralac, and Casin).
CDC42 family GTPases (RHOJ, RHOQ, CDC42) are linked to multiple human cancers and modulate cell-cycle progression, tumor cell migration/invasion, and tumor angiogenesis.

Physicochemical Properties

M.Wt 373.504
Formula C23H27N5
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

N1,N1-dimethyl-N3-(6-phenyl-2-(piperidin-4-yl)pyrimidin-4-yl)benzene-1,3-diamine

References

1. Jahid S, et al. Cell Rep. 2022 Apr 5;39(1):110641.

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