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pan-Ras inhibitor 3144

Chemical Structure : pan-Ras inhibitor 3144

CAS No.: 1835283-94-7

pan-Ras inhibitor 3144 (Compound 3144)

Catalog No.: PC-62695Not For Human Use, Lab Use Only.

pan-Ras inhibitor 3144 (Compound 3144) is a multivalent small-molecule, pan-RAS inhibitor with Kd of 4.7/17/6.6/3.7 uM for KRAS G12D/KRAS wt/HRAS/NRAS respectively.

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Biological Activity

pan-Ras inhibitor 3144 (Compound 3144) is a multivalent small-molecule, pan-RAS inhibitor with Kd of 4.7/17/6.6/3.7 uM for KRAS G12D/KRAS wt/HRAS/NRAS respectively.
pan-Ras inhibitor 3144 shows weak bindinf for RRAS2 (Kd=24 uM) and no activity for other small GTPases in the RAS superfamily.
pan-Ras inhibitor 3144 exhibits lethality in cells partially dependent on expression of RAS proteins.
pan-Ras inhibitor 3144 has suitable ADME properties and displays anti-tumor activity in xenograft mouse of pancreatic cancer; orally bioavailable.

Physicochemical Properties

M.Wt 717.659
Formula C36H41Cl2F3N6O2
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-amino-N-(3-(5-((4-(2,6-dichlorobenzyl)piperazin-1-yl)methyl)-3-(4-(trifluoromethoxy)phenyl)-1H-indol-1-yl)propyl)piperidine-4-carboxamide

References

1. Welsch ME, et al. Cell. 2017 Feb 23;168(5):878-889.e29.

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