PF-04217903 mesylate|cas:956906-93-7|西域试剂

PF-04217903 mesylate,99.87%

产品编号：Bellancom-12017A| CAS NO：956906-93-7| 分子式：C₂₀H₂₀N₈O₄S| 分子量：468.49

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货号	价格	库存与货期
Bellancom-12017A	￥750.00	杭州北京（现货）
Bellancom-12017A	￥1100.00	杭州北京（现货）
Bellancom-12017A	￥3300.00	杭州北京（现货）
Bellancom-12017A	￥5940.00	杭州北京（现货）

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PF-04217903 mesylate

产品介绍

PF-04217903 mesylate 是一种高效的ATP竞争性 c-Met 激酶抑制剂，K_i 为 4.8 nM。PF-04217903 mesylate 相对于 208 个激酶显示出 1000 倍以上的选择性。具有抗血管生成特性。

生物活性

PF-04217903 mesylate is a potent ATP-competitive c-Met kinase inhibitor with K_i of 4.8 nM for human c-Met. PF-04217903 mesylate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties.

体外研究

PF-04217903 mesylate (0.1-10000 nM; 48-72 hours) inhibits proliferation of c-Met–amplified human GTL-16 gastric carcinoma and H1993 NSCLC cells with IC₅₀ values of 12 and 30 nM, respectively.
PF-04217903 mesylate induces apoptosis of GTL-16 cells (IC₅₀=31 nM) .
PF-04217903 mesylate also inhibits HGF-mediated cell migration and Matrigel invasion in several c-Met–overexpressing tumor cell lines such as human NCI-H441 lung carcinoma and HT29 colon carcinoma with IC50 values comparable with those for inhibition of c-Met phosphorylation in these cell lines (IC₅₀= 7-12.5 nM).
PF-04217903 mesylate displays similar potency to inhibit the activity of c-Met-H1094R, c-Met-R988C, and c-Met-T1010I with IC₅₀ of 3.1 nM, 6.4 nM, and 6.7 nM, respectively, but has no inhibitory activity against c-Met-Y1230C with IC₅₀ of >10 μM.

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

Cell Proliferation Assay

Cell Line:	GTL-16, H1993 cells
Concentration:	0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time:	48-72 hours
Result:	Inhibited proliferation of c-Met–amplified human GTL-16 gastric carcinoma and H1993 NSCLC cells with IC₅₀ values of 12 and 30 nM, respectively.

Apoptosis Analysis

Cell Line:	GTL-16 cells
Concentration:	1.5-3333 nM
Incubation Time:	48 hours
Result:	Induced apoptosis of GTL-16 cells (IC₅₀=31 nM).

体内研究
(In Vivo)

PF-04217903 mesylate (1-30 mg/kg; p.o.; daily for 16 days) shows dose-dependent tumor growth inhibition, which correlated with the inhibition in c-Met phosphorylation in these tumors .
PF-04217903 mesylate (5-50 mg/kg, p.o.; once daily for 3 days) dose dependently inhibits c-Met, Gab-1, Erk1/2, and AKT phosphorylation and induced apoptosis (cleaved caspase-3) in U87MG xenograft tumors at all dose levels. PF-04217903 mesylate shows a significant dose-dependent reduction of human IL-8 levels in both the U87MG and GTL-16 models and decreases human VEGFA levels in the GTL-16 model. PF-04217903 mesylate strongly induces phospho-PDGFRβ levels in U87MG xenograft tumors.

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

Animal Model:	Female nu/nu mice GTL-16 xenograft model
Dosage:	1, 3, 10, 30 mg/kg
Administration:	Oral; daily for 16 days
Result:	Showed dose-dependent tumor growth inhibition, and was correlated with the inhibition in c-Met phosphorylation in these tumors.

体内研究

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

Animal Model:	Female nu/nu mice GTL-16 xenograft model
Dosage:	1, 3, 10, 30 mg/kg
Administration:	Oral; daily for 16 days
Result:	Showed dose-dependent tumor growth inhibition, and was correlated with the inhibition in c-Met phosphorylation in these tumors.

体内研究

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

Animal Model:	Female nu/nu mice GTL-16 xenograft model
Dosage:	1, 3, 10, 30 mg/kg
Administration:	Oral; daily for 16 days
Result:	Showed dose-dependent tumor growth inhibition, and was correlated with the inhibition in c-Met phosphorylation in these tumors.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (106.73 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1345 mL	10.6726 mL	21.3452 mL
5 mM	0.4269 mL	2.1345 mL	4.2690 mL
10 mM	0.2135 mL	1.0673 mL	2.1345 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 (sealed storage, away from moisture)。-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: ≥ 3 mg/mL (6.40 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (6.40 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 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% corn oil
Solubility: ≥ 3 mg/mL (6.40 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (6.40 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 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。