Super-TDU

Super-TDU; 纯度: 98.85%

Super-TDU 是一种特异性的 YAP 拮抗剂,可以靶向 YAP-TEAD 相互作用。Super-TDU 可以抑制胃癌小鼠模型的肿瘤生长。

Super-TDUamp;;

Super-TDU Chemical Structure

CAS No. : 1599441-71-0

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生物活性

Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model[1].

体外研究
(In Vitro)

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/cA nu/nu mice[1]
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[1]
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

Formula

C237H370N66O69S

CAS 号

1599441-71-0

Sequence Shortening

SVDDHFAKSLGDTWLQIGGSGNPKTANVPQTVPMRLRKLPDSFFKPPE

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

H2O : 50 mg/mL (9.47 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.1894 mL 0.9470 mL 1.8940 mL
5 mM 0.0379 mL 0.1894 mL 0.3788 mL
10 mM

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Jiao S, et al. A peptide mimicking VGLL4 function acts as a YAP antagonist therapy against gastric cancer. Cancer Cell. 2014 Feb 10;25(2):166-80.