Pan-RAS-IN-1是一种pan-Ras抑制剂，破坏Ras蛋白及其作用子的相互作用。
CAS：1835283-94-7
分子式：C36H41Cl2F3N6O2
分子量：717.65
纯度：98%
存储：Store at -20°C

Background:

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].

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