APS6-45

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APS6-45  纯度: 99.92%

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。

APS6-45

APS6-45 Chemical Structure

CAS No. : 2188236-41-9

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生物活性

APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity[1].

体外研究
(In Vitro)

APS6-45 (3-30 nM; 3 weeks) strongly suppresses TT human Medullary Thyroid Carcinoma (MTC) cells colony formation in a soft agar assay[1].
APS6-45 (1 μM; 1 h) strongly inhibits RAS pathway activity signaling in human MTC cell lines TT and MZ-CRC-1[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

APS6-45 (10 mg/kg; p.o. daily for 30 d) inhibits growth of TT tumors in mice and does not affect body weight[1].
APS6-45 (0.1-160 mg/kg; a single p.o.) does not cause detectable toxic effects in mice[1].
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[1].

上海金畔生物科技有限公司 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[1]
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)[1]
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.

分子量

548.39

Formula

C23H16F8N4O3
CAS 号

2188236-41-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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