AZ5104
(Synonyms: 奥西替尼中间体) 目录号 : GC12955
An active metabolite of AZD 9291
Cas No.:1421373-98-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Cell experiment: |
Cells were treated for 2 h with a dose-response of each drug (AZ-5104). Wild-type cells were stimulated for 10 minutes with 25 ng/mL of EGF before lysis. Level of EGFR phosphorylation was quantified in cell extracts using ELISA[1]. |
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References: [1]. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. |
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AZ5104, is the demethylated metabolite of AZD-9291,is a potent EGFR inhibitor. IC50 <1 nM, 6 nM, 1 nM, 25 nM, for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively.
EGFR (epidermal growth factor receptor) is a receptor tyrosine kinase on the cell surface. The receptor activation leads to dimerization and tyrosine autophosphorylation. It induces downstream cellular responses such as modification in gene expression, cell proliferation and cytoskeletal rearrangement etc.
Compare to AZD9291, AZ5104 has somewhat more potency in mutant EGFR cell lines ex19del (2 nmol/L in PC-9), T790M (2 nmol/L in H1975), and wild-type EGFR (33 nmol/L in LOVO) cell lines. In a phenotypic assay, AZ5104 showed a greater potency across cell lines in a phenotypic assay.
3 hours after oral dosing in the mouse, the circulating active metabolites in plasma is 33% for AZ5104. In both C/L858R and C/L+T mice, 5 mg/kg/day dose of AZ5104, also show efficacy in shrinking tumors.
Reference:
1. Cross DA, Ashton SE, Ghiorghiu S et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61.
| Cas No. | 1421373-98-9 | SDF | |
| 别名 | 奥西替尼中间体 | ||
| 化学名 | (Z)-N-(5-((4-(1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylimidic acid | ||
| Canonical SMILES | C=C/C(O)=N/C1=CC(NC2=NC=CC(C3=CNC4=CC=CC=C34)=N2)=C(OC)C=C1N(CCN(C)C)C | ||
| 分子式 | C27H31N7O2 | 分子量 | 485.58 |
| 溶解度 | ≥ 16.95mg/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。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0594 mL | 10.297 mL | 20.5939 mL |
| 5 mM | 0.4119 mL | 2.0594 mL | 4.1188 mL |
| 10 mM | 0.2059 mL | 1.0297 mL | 2.0594 mL |
| 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 | 只 |
| 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 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。