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SCH772984

CAS No. : 942183-80-4

MCE 国际站：SCH772984

产品活性：SCH772984 是一种高选择性和 ATP 竞争性 ERK 抑制剂，对 ERK1 和 ERK2 的 IC₅₀ 分别为 4 和 1 nM。SCH772984 在对天然 MAPK 抑制和耐药 MAPK 抑制的细胞中的 BRAF 或 RAS 突变，具有抗肿瘤活性。

研究领域：MAPK/ERK Pathway  |  Stem Cell/Wnt

作用靶点：ERK

In Vitro: SCH772984 (300 nM; 24-48hours) results in a G1 arrest in SCH772984-sensitive melanoma cells.
SCH772984 (3-300 nM; 24 hours) inhibits ERK and RSK phosphorylation.
SCH772984 shows EC₅₀ values less than 500 nM in approximately 88% and 49% of BRAF-mutant (n=25) or RAS-mutant (n=35) tumor lines, respectively.

In Vivo: SCH772984 (12.5-50 mg/kg; i.p.; twice daily for 14 days) leads to 98% tumor regression.
Dose-dependent antitumor activity is also observed in the KRAS-mutant pancreatic MiaPaCa model, with 36% regression at 50 mg/kg twice daily. Importantly, tumor regression is accompanied by robust inhibition of ERK phosphorylation in tumor tissue. SCH772984 is well tolerated on this schedule as measured by morbidity, lethality, or body weight loss.

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