VT103|cas:2290608-13-6|西域试剂

VT103,99.26%

产品编号：Bellancom-134955| CAS NO：2290608-13-6| 分子式：C₁₈H₁₇F₃N₄O₂S| 分子量：410.41

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货号	价格	库存与货期
Bellancom-134955	￥4000.00	杭州北京（现货）
Bellancom-134955	￥6800.00	杭州北京（现货）
Bellancom-134955	￥13500.00	杭州北京（现货）

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VT103

产品介绍

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。

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.

体外研究

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.
VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1.
VT103 shows an IC₅₀ of 1.02 nM in YAP reporter assay.

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

体内研究

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

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 (%)	C_max (ng/mL)	C₂₄ hours (ng/mL)
7 mg/kg	13.2	4.5	4.7	20.0	14.9	75	896 (1 hour)	340

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

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

体内研究

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

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 (%)	C_max (ng/mL)	C₂₄ hours (ng/mL)
7 mg/kg	13.2	4.5	4.7	20.0	14.9	75	896 (1 hour)	340

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

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

性状

Solid

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.09 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。