VT103

VT103

V650841-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

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

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

2290608-13-6

C18H17F3N4O2S

410.41 g/mol

137534047

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

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

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

LLCVDQHLYHBAHR-UHFFFAOYSA-N

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

137534047

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

2

8

5

410.102 Da

410.102 Da

84.400 Ų

28

0

617

0

1

3.1