APS6-45|cas:2188236-41-9|西域试剂

APS6-45,99.58%

产品编号：Bellancom-124944| CAS NO：2188236-41-9| 分子式：C₂₃H₁₆F₈N₄O₃| 分子量：548.39

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-124944	￥2500.00	杭州北京（现货）
Bellancom-124944	￥4200.00	杭州北京（现货）
Bellancom-124944	￥7900.00	杭州北京（现货）
Bellancom-124944	￥12000.00	杭州北京（现货）

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APS6-45

产品介绍

APS6-45 是一种口服活性的肿瘤校准抑制剂 (TCI)。APS6-45 抑制 RAS/MAPK 信号传导并表现出抗肿瘤活性。

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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), C_max (9.7 µM) and AUC_0-24 (123.7 µM•h) in mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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:	T_1/2=5.6 h, C_max=9.7 µM, AUC_0-24=123.7 µM•h.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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:	T_1/2=5.6 h, C_max=9.7 µM, AUC_0-24=123.7 µM•h.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (455.88 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8235 mL	9.1176 mL	18.2352 mL
5 mM	0.3647 mL	1.8235 mL	3.6470 mL
10 mM	0.1824 mL	0.9118 mL	1.8235 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.79 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.79 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。