Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model.
体外研究
Super-TDU downregulates expression of YAP-TEADs target genes CTGF, CYR61, and CDX2. Super-TDU inhibits cell viability and colony formation of GC cell lines MGC-803, BGC-823, and HGC27.
体内研究
Super-TDU (intravenous injection; 50 μg/kg or 500 μg/kg; per day) markedly decreases the sizes, weights of tumors, and YAP target genes in a dose-dependent manner in mice.
Super-TDU (intravenous injection; 250 μg/kg 500 μg/kg) has the t1/2α of 0.78 hours and 0.82 hours; the Cmax of 6.12 ng/mL and 13.3 ng/mL; the CL of 7.41 ml/min/kg and 7.72 ml/min/kg for 250 μg/kg and 500 μg/kg in mice, respectively.
Animal Model:
BALB/cA nu/nu mice
Dosage:
50 μg/kg or 500 μg/kg
Administration:
Intravenous Injection; per day
Result:
Decreased the sizes, weights of tumors, and YAP target genes in a dose-dependent manner.
Animal Model:
BALB/cA nu/nu mice
Dosage:
250 μg/kg or 500 μg/kg (Pharmacokinetic Study)
Administration:
Intravenous Injection
Result:
The t1/2α is 0.78 hours and 0.82 hours; the Cmax is 6.12 ng/mL and 13.3 ng/mL; the CL is7.41 ml/min/kg and 7.72 ml/min/kg for 250 μg/kg and 500 μg/kg in mice, respectively.
分子量
5279.94
CAS号
1599441-71-0
运输条件
Room temperature in continental US; may vary elsewhere.