Pan-RAS-IN-1

For research use only. Not for therapeutic Use.

  • CAT Number: I020674
  • CAS Number: 1835283-94-7
  • Molecular Formula: C36H41Cl2F3N6O2
  • Molecular Weight: 717.65
  • Purity: ≥95%
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Pan-RAS-IN-1 is a pan-Ras inhibitor that disrupts the interaction of Ras proteins and their effectors.
Pan-RAS-IN-1 binds to KRasG12D-GppNHp with an affinity less than 20 μM. Pan-RAS-IN-1 binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins. The potency of pan-RAS-IN-1 correlates with the degree of dependency on the mutated isoform over a 5-fold concentration range. At some concentrations, pan-RAS-IN-1 is cytostatic, possibly due to pan-RAS inhibition. Pan-RAS-IN-1 is evaluated in primary T cell acute lymphoblastic leukemia (T-ALL) cells. Selective lethality is observed, with mutant NRAS cells retaining only 20%-40% viability after 5 μM treatment[1].
Pan-RAS-IN-1 administration results in inhibition of tumor growth over 15 days of treatment. Pan-RAS-IN-1-treated mice exhibits decreased tumor pERK levels compared with vehicle treated mice. A modest increase in cleaved caspase-3 is also observed, showing that in this model, pan-RAS-IN-1 has the capacity to induce caspase activation[1].


Catalog Number I020674
CAS Number 1835283-94-7
Synonyms

4-amino-N-[3-[5-[[4-[(2,6-dichlorophenyl)methyl]piperazin-1-yl]methyl]-3-[4-(trifluoromethoxy)phenyl]indol-1-yl]propyl]piperidine-4-carboxamide

Molecular Formula C36H41Cl2F3N6O2
Purity ≥95%
InChI InChI=1S/C36H41Cl2F3N6O2/c37-31-3-1-4-32(38)30(31)23-46-19-17-45(18-20-46)22-25-5-10-33-28(21-25)29(26-6-8-27(9-7-26)49-36(39,40)41)24-47(33)16-2-13-44-34(48)35(42)11-14-43-15-12-35/h1,3-10,21,24,43H,2,11-20,22-23,42H2,(H,44,48)
InChIKey GMDFJPPJWWJNKF-UHFFFAOYSA-N
SMILES C1CNCCC1(C(=O)NCCCN2C=C(C3=C2C=CC(=C3)CN4CCN(CC4)CC5=C(C=CC=C5Cl)Cl)C6=CC=C(C=C6)OC(F)(F)F)N
Reference

[1]. Welsch ME, et al. Multivalent Small-Molecule Pan-RAS Inhibitors. Cell. 2017 Feb 23;168(5):878-889.e29.
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