产品
编 号：F750915
分子式：C18H17F3N4O2S
分子量：410.41
分子式：C18H17F3N4O2S
分子量：410.41
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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询价
结构图
CAS No: 2290608-13-6
产品详情
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 miceDoseIVPO
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)
13.24.54.720.014.975896 (1 hour)340
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.
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 miceDoseIVPO
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)
13.24.54.720.014.975896 (1 hour)340
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.
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