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编 号:F285528
分子式:C21H31N5O2
分子量:385.5
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5mg
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10mg
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50mg
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100mg
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生物活性:
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM.

体内研究:
ZT-12-037-01 (腹腔注射;25-50 mg/kg;每日一次;21 天) 抑制 SK-MEL-2 异种移植黑色素瘤的生长,肿瘤切片表明通过增加裂解的 caspase-3 诱导细胞凋亡。Animal Model:SK-MEL-2 xenograft melanoma nude mice with hTERT/p53DD/CDK4(R24C) melanocytes
Dosage:25 mg/kg; 50 mg/kg
Administration:Intraperitoneally injection; 21 days; once a day
Result:Inhibited growth of SK-MEL-2 xenograft melanoma.

体外研究:
ZT-12-037-01 (3 μM;14 天) 显著抑制突变的 NRAS-STK19 驱动的黑色素细胞集落形成和增殖。 ZT-12-037-01 (0-3 μM) 具有 ZT-12-037-01 对HPMs中STK19WT和STK19D89N激活的NRAS磷酸化的抑制作用。
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