货号	规格	价格	上海	北京	珠海	重庆	武汉
S89149-5mg买3赠1	99.70%	￥750.00 S89149-5mg ￥750.00 现货（买3赠1）	5 5	-	-	-	-
S89149-10mg促销	99.70%	￥1200.00 ￥960.00 S89149-10mg ￥960.00 现货	6 6	-	-	-	-
S89149-25mg促销	99.70%	￥2400.00 ￥1920.00 S89149-25mg ￥1920.00 现货	5 5	-	-	-	-
S89149-100mg促销	≥98%	￥5080.00 ￥4060.00 S89149-100mg ￥4060.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity

靶点：

Ras;MAPK; Ras

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

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.

参考文献：

1. Sonoshita M, et, al. A whole-animal platform to advance a clinical kinase inhibitor into new disease space. Nat Chem Biol. 2018 Mar;14(3):291-298.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.824 ml	9.118 ml	18.235 ml
5 mM	0.365 ml	1.824 ml	3.647 ml
10 mM	0.182 ml	0.912 ml	1.824 ml
50 mM	0.036 ml	0.182 ml	0.365 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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