产品
编 号：F276493
分子式：C23H16F8N4O3
分子量：548.39
分子式：C23H16F8N4O3
分子量：548.39
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 2188236-41-9
产品详情
生物活性：
APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.
体内研究：
APS6-45 (10 mg/kg; p.o. daily for 30 d) inhibits growth of TT tumors in mice and does not affect body weight.APS6-45 (0.1-160 mg/kg; a single p.o.) does not cause detectable toxic effects in mice.APS6-45 (20 mg/kg; a single p.o.) exhibits long half-life (5.6 h), Cmax (9.7 μM) and AUC0-24 (123.7 μM?h) in mice.Animal Model:Female nude mice (6 weeks) are implanted with TT cells
Dosage:10 mg/kg
Administration:P.o. daily for 30 days
Result:Led to partial or complete responses in 75% and was well tolerated.
Animal Model:Male ICR mice (6 weeks of age)
Dosage:20 mg/kg (Pharmacokinetic Analysis)
Administration:A single p.o.
Result:T1/2=5.6 h, Cmax=9.7 μM,AUC0-24=123.7 μM?h.
体外研究：
APS6-45 (3-30 nM; 3 weeks) strongly suppresses TT human Medullary Thyroid Carcinoma (MTC) cells colony formation in a soft agar assay.APS6-45 (1 μM; 1 h) strongly inhibits RAS pathway activity signaling in human MTC cell lines TT and MZ-CRC-1.
APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.
体内研究：
APS6-45 (10 mg/kg; p.o. daily for 30 d) inhibits growth of TT tumors in mice and does not affect body weight.APS6-45 (0.1-160 mg/kg; a single p.o.) does not cause detectable toxic effects in mice.APS6-45 (20 mg/kg; a single p.o.) exhibits long half-life (5.6 h), Cmax (9.7 μM) and AUC0-24 (123.7 μM?h) in mice.Animal Model:Female nude mice (6 weeks) are implanted with TT cells
Dosage:10 mg/kg
Administration:P.o. daily for 30 days
Result:Led to partial or complete responses in 75% and was well tolerated.
Animal Model:Male ICR mice (6 weeks of age)
Dosage:20 mg/kg (Pharmacokinetic Analysis)
Administration:A single p.o.
Result:T1/2=5.6 h, Cmax=9.7 μM,AUC0-24=123.7 μM?h.
体外研究：
APS6-45 (3-30 nM; 3 weeks) strongly suppresses TT human Medullary Thyroid Carcinoma (MTC) cells colony formation in a soft agar assay.APS6-45 (1 μM; 1 h) strongly inhibits RAS pathway activity signaling in human MTC cell lines TT and MZ-CRC-1.
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