Home>>Signaling Pathways>> Cell Cycle/Checkpoint>> Aurora Kinase>>AMG-900

AMG-900 Sale

目录号 : GC13198

A selective pan-Aurora kinase inhibitor

AMG-900 Chemical Structure

Cas No.:945595-80-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥924.00
现货
5mg
¥777.00
现货
10mg
¥1,334.00
现货
50mg
¥3,990.00
现货
200mg
¥10,374.00
现货
500mg
¥26,040.00
现货
1g
¥36,330.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Kinase experiment [1]:

Enzyme kinase assays

Recombinant GST- or His-tagged aurora-A (TPX2), and aurora-B proteins were expressed using a baculovirus system and purified by affinity chromatography. AMG 900 activity was assessed using a standardized homogenous time-resolved fluorescence (HTRF) assay. Enzyme assays for 24 other kinases (aurora-C, p38α, TYK2, JNK2, JAK3, c-Met, VEGFR2, p38β, TIE-2, ABL (T315I), ERK1, BTK, JNK3, CDK5, PKAα, JNK1, p70S6K, PKBα, MSK1, LCK, SRC, IGFR, JAK2, and c-KIT) were done internally in a similar manner. Concentrations of enzyme, peptide substrate, and ATP in the reaction were optimized depending on the specific activity of the kinase and measured Km values for their corresponding substrates. AMG 900 was evaluated in a kinome competition binding assay (n = 353 unique kinases) by Ambit Biosciences. AMG 900 was initially screened at a single concentration of 1000 nM, and quantitative binding constants (Kd) were determined for each positive hit (< 20 percentage of control).

Cell experiment [1]:

Cell lines

Human colon carcinoma HCT116 cell line

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months.

Reaction Conditions

50 nM; 48 hrs

Applications

AMG 900 time-dependently increased apoptosis through the induction of cleaved caspase-7.

Animal experiment [1]:

Animal models

Nude mice bearing HCT116 tumors

Dosage form

3.75, 7.5 or 15 mg/kg; o.p.; 3, 6 or 9 hrs

Applications

AMG 900 significantly inhibited HCT116 tumors in a dose-dependent manner.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Payton, M., et al., Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res, 2010. 70(23): p. 9846-54.

产品描述

AMG900 is a highly sensitive and orally bioavailable inhibitor of Aurora Kinase with IC50 values of 5 nmol/L.

AMG900 is an inhibitor of all three aurora kinase family members. It was founded through the discovery of a new class of ATP-competitive phtha-lazinamine small molecule inhibitors of aurora kinases. AMG900 inhibits autophosphorylation of aurora-A and aurora-B in tumor cells, and also aborts cell division without a prolonged mitosis arrest and finally results cell death. It can inhibit 26 different tumor cell lines proliferation, meanwhile, it also has the ability to enhance other aurora kinase inhibitors' effective. [1, 2]

AMG900 had been tested in animal level using mice models. Mice bearing established HCT116 tumors and orally delivery AMG900. Comparing to the vehicle group, the experiment groups delivery AMG900 with different concentration showed an obvious smaller tumor volume. These results revealed that AMG900 has the ability to significantly inhibit tumor growth.

References:
1.  Payton, M., et al., Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res, 2010. 70(23): p. 9846-54.
2.  Geuns-Meyer, S., et al., Discovery of N-(4-(3-(2-Aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4- (4-methylthiophen-2-yl)p hthalazin-1-amine (AMG 900), A Highly Selective, Orally Bioavailable Inhibitor of Aurora Kinases with Activity against Multidrug-Resistant Cancer Cell Lines. J Med Chem, 2015. 58(13): p. 5189-207.

Chemical Properties

Cas No. 945595-80-2 SDF
化学名 N-[4-[3-(2-aminopyrimidin-4-yl)pyridin-2-yl]oxyphenyl]-4-(4-methylthiophen-2-yl)phthalazin-1-amine
Canonical SMILES CC1=CSC(=C1)C2=NN=C(C3=CC=CC=C32)NC4=CC=C(C=C4)OC5=C(C=CC=N5)C6=NC(=NC=C6)N
分子式 C28H21N7OS 分子量 503.58
溶解度 ≥ 25.2 mg/mL in DMSO 储存条件 Store at -20°C
General tips 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.9858 mL 9.9289 mL 19.8578 mL
5 mM 0.3972 mL 1.9858 mL 3.9716 mL
10 mM 0.1986 mL 0.9929 mL 1.9858 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置