Savolitinib(Synonyms: 赛沃替尼; Volitinib; HMPL-504; AZD-6094)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Savolitinib (Synonyms: 赛沃替尼; Volitinib; HMPL-504; AZD-6094) 纯度: 99.56%

Savolitinib (AZD-6094) 是一种高效选择性、口服生物利用度 c-Met 抑制剂,对 c-Met 和 p-Met 的 IC50 分别为 5 nM 和 3 nM。Savolitinib (AZD-6094) 以 ATP 竞争的方式选择性结合并抑制 c-Met 的激活,破坏 c-Met 信号转导途径。具有抗肿瘤活性。

Savolitinib(Synonyms: 赛沃替尼; Volitinib;  HMPL-504;  AZD-6094)

Savolitinib Chemical Structure

CAS No. : 1313725-88-0

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10 mM * 1 mL in DMSO ¥1899 In-stock
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生物活性

Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity[1][2].

IC50 & Target

IC50: 5 nM (c-Met) and 3 nM (p-Met)[1]

体内研究
(In Vivo)

Savolitinib (Compound 28; 1-10.0 mg/kg; oral administration; daily; for 21 days; athymic nude mice) demonstrates dose-dependent tumor growth inhibition in a U87MG subcutaneous xenograft model. In addition, none of the mice in the dosing groups exhibits body weight loss during the experiment[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: U87MG xenograft model in athymic nude mice[1]
Dosage: 1 mg/kg, 2.5 mg/kg and 10.0 mg/kg
Administration: Oral administration; daily; for 21 days
Result: Demonstrated dose-dependent tumor growth inhibition in a U87MG subcutaneous xenograft model.

Clinical Trial

分子量

345.36

Formula

C17H15N9

CAS 号

1313725-88-0

中文名称

赛沃替尼;沃利替尼

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 : 25 mg/mL (72.39 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8955 mL 14.4776 mL 28.9553 mL
5 mM 0.5791 mL 2.8955 mL 5.7911 mL
10 mM 0.2896 mL 1.4478 mL 2.8955 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    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (6.02 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.02 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (6.02 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (6.02 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.02 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.02 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]. Jia H, et al. Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical development for treatment of cancer. J Med Chem. 2014 Sep 25;57(18):7577-89.

    [2]. Gavine PR, et al. Volitinib, a potent and highly selective c-Met inhibitor, effectively blocks c-Met signaling and growth in c-MET amplified gastric cancer patient-derived tumor xenograft models. Mol Oncol. 2015 Jan;9(1):323-33.

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