S49076|cas:1265965-22-7|西域试剂

S49076,99.71%

产品编号：Bellancom-12965| CAS NO：1265965-22-7| 分子式：C₂₂H₂₂N₄O₄S| 分子量：438.50

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-12965	￥600.00	杭州北京（现货）
Bellancom-12965	￥950.00	杭州北京（现货）
Bellancom-12965	￥1200.00	杭州北京（现货）
Bellancom-12965	￥3900.00	杭州北京（现货）
Bellancom-12965	￥7100.00	杭州北京（现货）

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S49076

产品介绍

S49076是新颖高效的MET, AXL/MER和FGFR1/2/3抑制剂， IC₅₀值小于20 nM。

生物活性

S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC₅₀ values below 20 nM.

体外研究

S49076 potently blocks cellular phosphorylation of MET, AXL, and FGFRs and inhibits downstream signaling. S49076 inhibits the proliferation of MET- and FGFR2-dependent gastric cancer cells, blocks MET-driven migration of lung carcinoma cells, and inhibits colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. Total inhibition of MET phosphorylation is seen after 2 hours of incubation with 10 nM S49076 and an with an IC₅₀ of 2 nM. S49076 inhibits MET phosphorylation on this site in GTL-16 gastric carcinoma cells with an IC₅₀ value of 3 nM. The IC₅₀ for AXL inhibition by S49076 is 56 nM. S49076 inhibits AXL signaling via AKT with an IC₅₀ of 33 nM.

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

体内研究

In tumor xenograft models, a good pharmacokinetic/pharmacodynamic relationship for MET and FGFR2 inhibition following oral administration of S49076 is established and correlated well with impact on tumor growth. MET, AXL, and the FGFRs have all been implicated in resistance to VEGF/VEGFR inhibitors such as bevacizumab. Combination of S49076 with bevacizumab in colon carcinoma xenograft models leads to near total inhibition of tumor growth. S49076 alone caused tumor growth arrest in bevacizumab-resistant tumors.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 31 mg/mL (70.70 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2805 mL	11.4025 mL	22.8050 mL
5 mM	0.4561 mL	2.2805 mL	4.5610 mL
10 mM	0.2281 mL	1.1403 mL	2.2805 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: ≥ 2.5 mg/mL (5.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.70 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.70 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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