VT103

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

VT103 

VT103 是 VT101 的类似物，是一种具有口服活性和选择性的 TEAD1 蛋白棕榈酰化抑制剂。 VT103 抑制 YAP/TAZ-TEAD 促进的基因转录，阻断 TEAD auto-palmitoylation，阻断 YAP/TAZ和TEAD 之间的相互作用。VT103 可用于癌症研究。

VT103

VT103 Chemical Structure

CAS No. : 2290608-13-6

规格 价格 是否有货
5 mg ￥4000 询问价格 & 货期
10 mg ￥6800 询问价格 & 货期
25 mg ￥13500 询问价格 & 货期

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生物活性

VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer[1].

IC50 & Target

TEAD1 Palmitoylation[1]
体外研究
(In Vitro)

VT103 (HEK293T cells; 3 μM) appeares to be TEAD1-selective, as it does not block palmitoylation of TEAD2, TEAD3, or TEAD4. VT103 (NF2-deficient NCI-H226 cells; 3 mmol/L; 4 or 24 hours) selectively disrupts YAP–TEAD1 interaction[1].
VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1[1].
VT103 shows an IC50 of 1.02 nM in YAP reporter assay[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

VT103 (0.3~10 mg/kg; p.o. once per day) blocks tumor growth even at 0.3 mg/kg[1].
Pharmacokinetics of VT103 in mice[1]

Dose IV PO
7 mg/kg T1/2 (hours) Vdss (L/kg) CI(mL/min/kg) AUC 0-24 hours (μg*h/mL) AUC 0-24 hours (μg*h/mL) Oral availability (%) Cmax (ng/mL) C24 hours (ng/mL)
13.2 4.5 4.7 20.0 14.9 75 896 (1 hour) 340

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NCI-H226-tumor bearing mice[1]
Dosage: 0.3~10 mg/kg
Administration: P.o. once per day
Result: Blocked tumor growth even at 0.3 mg/kg.

分子量

410.41

Formula

C18H17F3N4O2S
CAS 号

2290608-13-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (121.83 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4366 mL 12.1829 mL 24.3659 mL
5 mM 0.4873 mL 2.4366 mL 4.8732 mL
10 mM 0.2437 mL 1.2183 mL 2.4366 mL

*

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]. Tang TT, et al. Small Molecule Inhibitors of TEAD Auto-palmitoylation Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. Mol Cancer Ther. 2021;20(6):986-998.

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