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Pan-RAS-IN-1

CAS No. : 1835283-94-7

MCE 站：Pan-RAS-IN-1

产品活性：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。

研究领域：GPCR/G Protein

作用靶点：Ras

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.

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.

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