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SCH772984 HCl 是一种特异性的 ERK1/2 抑制剂,具有 I 型和 II 型激酶抑制剂的特性,其 IC50 分别为 4 和 1 nM。 SCH772984 HCl 在 BRAF、NRAS 或 KRAS 突变的肿瘤细胞中具有纳摩尔级细胞效力,并诱导肿瘤消退。 SCH772984 HCl 可用于 MAPK 抑制剂难治性肿瘤的研究。
SCH772984 HCl 是一种特异性的 ERK1/2 抑制剂,具有 I 型和 II 型激酶抑制剂的特性,其 IC50 分别为 4 和 1 nM。 SCH772984 HCl 在 BRAF、NRAS 或 KRAS 突变的肿瘤细胞中具有纳摩尔级细胞效力,并诱导肿瘤消退。 SCH772984 HCl 可用于 MAPK 抑制剂难治性肿瘤的研究。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 912 | 期货 | |
5 mg | ¥ 1,389 | 期货 | |
10 mg | ¥ 1,797 | 期货 |
产品描述 | SCH772984 HCl is a selective inhibitor of ERK1/2 that displays behaviors of both type I and type II kinase inhibitors, with IC50s of 4 and 1 nM, respectively. SCH772984 HCl has nanomolar cellular potency in tumor cells with mutations in BRAF, NRAS, or KRA |
靶点活性 | ERK1:4 nM, ERK2:1 nM |
体外活性 | In LOX BRAFV600E melanoma cells, SCH772984 HCl (3, 10, 30, 100, 300 nM; 24 hours) inhibited ERK and RSK phosphorylation. SCH772984 HCl showed 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 SCH772984 HCl-sensitive melanoma cells, SCH772984 HCl (300 nM; 24-48hours) resulted in a G1 arrest[1]. |
体内活性 | In female nude mice bearing human LOX BRAFV600E tumors, SCH772984 HCl (12.5, 25, 50 mg/kg; i.p. twice daily for 14 days) lead to 98% tumor regression at all doses. 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[1]. |
分子量 | 624.14 |
分子式 | C33H34ClN9O2 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | H2O: 23.5 mg/mL (with gentle warming) |
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