pan-Ras inhibitor 3144( Compound 3144 )

Catalog No. M12834 CAS No. 1835283-94-7

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Product Name

pan-Ras inhibitor 3144
Note

Research use only, not for human use.
Brief Description

pan-Ras inhibitor 3144 (Compound 3144) is a multivalent small-molecule, pan-RAS inhibitor.
Description

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; shows weak bindinf for RRAS2 (Kd=24 uM) and no activity for other small GTPases in the RAS superfamily; exhibits lethality in cells partially dependent on expression of RAS proteins; has suitable ADME properties and displays anti-tumor activity in xenograft mouse of pancreatic cancer; orally bioavailable.
Synonyms

Compound 3144
Pathway

MAPK/ERK Signaling
Target

Ras
Recptor

Ras
Research Area

——
Indication

——

CAS Number

1835283-94-7
Formula Weight

717.66
Molecular Formula

C36H41Cl2F3N6O2
Purity

99.5% (LCMS)
Solubility

DMSO : ≥ 50 mg/mL 69.67 mM
SMILES

O=C(C1(N)CCNCC1)NCCCN2C=C(C3=CC=C(OC(F)(F)F)C=C3)C4=C2C=CC(CN5CCN(CC6=C(Cl)C=CC=C6Cl)CC5)=C4
Chemical Name

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

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

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