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Product details

名称

VT103

英文名称

VT103

货号

V650841-5mg

包装规格

5mg

浓度

≥99%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

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 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. VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1. VT103 shows an IC 50 of 1.02 nM in YAP reporter assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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) C 24 hours (ng/mL) 13.2 4.5 4.7 20.0 14.9 75 896 (1 hour) 340 MCE 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. Form:Solid IC50& Target:TEAD1 Palmitoylation

生化机理

VT103 是 VT101 的类似物，是一种口服活性和选择性 TEAD1 蛋白棕榈酰化抑制剂。VT103 可抑制 YAP/TAZ-TEAD 促进的基因转录，阻止 TEAD 自身棕榈酰化，并破坏 YAP/TAZ 与 TEAD 之间的相互作用。VT103 可以

CAS号

2290608-13-6

分子式

C18H17F3N4O2S

分子量

410.41 g/mol

PubChem编号

137534047

Isomeric SMILES

CNS(=O)(=O)C1=CC(=C(C=C1)NC2=CC=C(C=C2)C(F)(F)F)C3=CN(C=N3)C

IIUPAC Name

N-methyl-3-(1-methylimidazol-4-yl)-4-[4-(trifluoromethyl)anilino]benzenesulfonamide

INCHI

1S/C18H17F3N4O2S/c1-22-28(26,27)14-7-8-16(15(9-14)17-10-25(2)11-23-17)24-13-5-3-12(4-6-13)18(19,20)21/h3-11,22,24H,1-2H3

InChi Key

LLCVDQHLYHBAHR-UHFFFAOYSA-N

Smiles

CNS(=O)(=O)C1=CC(=C(C=C1)NC2=CC=C(C=C2)C(F)(F)F)C3=CN(C=N3)C

PubChem CID

137534047

溶解性

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

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

410.102 Da

单同位素质量Monoisotopic Mass

410.102 Da

拓扑极表面积Topological Polar Surface Area

84.400 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

617

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

3.1

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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