Pan-RAS-IN-1

Pan-RAS-IN-1

P655191-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

Pan-RAS-IN-1 is a pan-Ras inhibitor that disrupts the interaction of Ras proteins and their effectors. In Vitro Pan-RAS-IN-1 binds to KRas G12D -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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Pan-RAS-IN-1 是一种泛 Ras 抑制剂，能破坏 Ras 蛋白与其效应物之间的相互作用。

1835283-94-7(DMSO)

C36H41Cl2F3N6O2

717.65 g/mol

O=C(C1(N)CCNCC1)NCCCN2C3=CC=C(CN4CCN(CC5=C(Cl)C=CC=C5Cl)CC4)C=C3C(C6=CC=C(OC(F)(F)F)C=C6)=C2