AMG-337|cas:1173699-31-4|西域试剂

AMG-337,99.43%

产品编号：Bellancom-18696| CAS NO：1173699-31-4| 分子式：C₂₃H₂₂FN₇O₃| 分子量：463.46

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货号	价格	库存与货期
Bellancom-18696	￥900.00	杭州北京（现货）
Bellancom-18696	￥1500.00	杭州北京（现货）
Bellancom-18696	￥2500.00	杭州北京（现货）
Bellancom-18696	￥4500.00	杭州北京（现货）
Bellancom-18696	￥7500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

AMG-337

产品介绍

AMG-337 是一种口服有效的选择性 MET 激酶抑制剂，抑制 WT MET、H1094R MET、M1250T MET、HGF-stimulated pMET (PC3 细胞) MET、V1092I MET、Y1230H MET 和 D1228H MET 的 IC₅₀ 值分别为 1、1、4.7、5、21.5、1077 和 >4000 nM。AMG 337 在 MET 扩增的癌细胞系中抑制 MET 及其下游效应子的磷酸化，从而抑制 MET 依赖的细胞增殖和诱导凋亡 (apoptosis)。

生物活性

AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC₅₀ values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis.

体外研究

AMG 337 (0-3 µM; 72 h) inhibits proliferation in MET-dependent cancer cell lines.
AMG 337 (0-300 nM; 0-24 h; MKN-45, SNU-620, and SNU-5 cells) inhibits signaling through the PI3K and MAPK pathways in MET-amplified gastric cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis.

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

Apoptosis Analysis

Cell Line:	MKN-45 and SNU-620 cells
Concentration:	0, 3, 10, 30, 100 and 300 nM
Incubation Time:	24 hours
Result:	Increased the number of cells undergoing apoptosis.

Cell Cycle Analysis

Cell Line:	MKN-45 and SNU-620 cells
Concentration:	0, 3, 10, 30, 100 and 300 nM
Incubation Time:	24 hours
Result:	Increased in a dose-dependent in cells in the G1 phase and with concurrent reduction of cells in S-phase.

Western Blot Analysis

Cell Line:	MKN-45, SNU-620, and SNU-5 cells
Concentration:	100 nM
Incubation Time:	2 hours
Result:	Inhibited MET phosphorylation and phosphorylation of downstream effectors.

Western Blot Analysis

Cell Line:	MKN-45, SNU-620, and SNU-5 cells
Concentration:	100 nM
Incubation Time:	24 hours
Result:	Induced PARP and caspase-3 cleavage in SNU-620 and SNU-5 cells.

体内研究
(In Vivo)

AMG 337 (0-30 mg/kg; p.o.; daily, for 28 d) inhibits MET signaling in tumor xenografts and inhibits tumor growth in MET-dependent tumor xenograft models.
AMG 337 (0-3 mg/kg; p.o.; once, for 3 or 24 h) is associated with increased necrosis in the MET-dependent SNU-620 tumor xenograft model.

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

Animal Model:	Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts
Dosage:	0, 0.3, and 1 mg/kg (SNU-620 xenograft); 0, 0.3, 1, 3, and 10 mg/kg (SNU-5 xenograft); 0, 3, 10 and 30 mg/kg (U-87 xenograft)
Administration:	Oral administration; daily, for 28 days
Result:	Inhibited tumor growth in MET-dependent tumor xenograft models.

Animal Model:	Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts
Dosage:	0.1, 0.5, 0.75, 1, 2, and 3 mg/kg
Administration:	Oral administration; once, for 3 hours
Result:	Inhibited Gab-1 phosphorylation in a dose-dependent manner.

Animal Model:	Female CD1 nu/nu mice with SNU-620 xenograft model (6-11 weeks of age; 20-26 g)
Dosage:	0, 0.3, 1, and 3 mg/kg
Administration:	Oral administration; once, for 3 or 24 hours
Result:	Increased immunohistochemical staining with anti-caspase-3 antibody and decreased immunohistochemical staining with anti-BrdU antibody.

体内研究

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

Animal Model:	Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts
Dosage:	0, 0.3, and 1 mg/kg (SNU-620 xenograft); 0, 0.3, 1, 3, and 10 mg/kg (SNU-5 xenograft); 0, 3, 10 and 30 mg/kg (U-87 xenograft)
Administration:	Oral administration; daily, for 28 days
Result:	Inhibited tumor growth in MET-dependent tumor xenograft models.

Animal Model:	Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts
Dosage:	0.1, 0.5, 0.75, 1, 2, and 3 mg/kg
Administration:	Oral administration; once, for 3 hours
Result:	Inhibited Gab-1 phosphorylation in a dose-dependent manner.

Animal Model:	Female CD1 nu/nu mice with SNU-620 xenograft model (6-11 weeks of age; 20-26 g)
Dosage:	0, 0.3, 1, and 3 mg/kg
Administration:	Oral administration; once, for 3 or 24 hours
Result:	Increased immunohistochemical staining with anti-caspase-3 antibody and decreased immunohistochemical staining with anti-BrdU antibody.

体内研究

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

Animal Model:	Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts
Dosage:	0, 0.3, and 1 mg/kg (SNU-620 xenograft); 0, 0.3, 1, 3, and 10 mg/kg (SNU-5 xenograft); 0, 3, 10 and 30 mg/kg (U-87 xenograft)
Administration:	Oral administration; daily, for 28 days
Result:	Inhibited tumor growth in MET-dependent tumor xenograft models.

Animal Model:	Female CD1 nu/nu mice bearing SNU-620, SNU-5, or U-87 MG xenografts
Dosage:	0.1, 0.5, 0.75, 1, 2, and 3 mg/kg
Administration:	Oral administration; once, for 3 hours
Result:	Inhibited Gab-1 phosphorylation in a dose-dependent manner.

Animal Model:	Female CD1 nu/nu mice with SNU-620 xenograft model (6-11 weeks of age; 20-26 g)
Dosage:	0, 0.3, 1, and 3 mg/kg
Administration:	Oral administration; once, for 3 or 24 hours
Result:	Increased immunohistochemical staining with anti-caspase-3 antibody and decreased immunohistochemical staining with anti-BrdU antibody.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (215.77 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1577 mL	10.7884 mL	21.5768 mL
5 mM	0.4315 mL	2.1577 mL	4.3154 mL
10 mM	0.2158 mL	1.0788 mL	2.1577 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 (5.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.39 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 (5.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.39 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.39 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。