AZD2932
目录号 : GC17959
A multi-kinase inhibitor
Cas No.:883986-34-3
Sample solution is provided at 25 µL, 10mM.
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AZD2932 is a potent inhibitor for multiple protein tyrosine kinases (IC50 = 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.) [1]
VEGFR are receptors for vascular endothelial growth factor and belong to receptor tyrosine kinases. It mediates in various cellular functions, including endothelial proliferation, migration, survival, tubular morphogenesis and sprouting. PDGFR are platelet-derived growth factor receptors that exhibit intracellular tyrosine kinase activity. It involves in embryonic development, angiogenesis, proliferation and differentiation etc.
AZD2932 has a potent and balanced profile against PDGFR, VEGFR-2, Flt-3 and c-Kit (IC50: 0.009). It also has a good fraction unbound between 3.3% free in human and 7.0% in dog sera and has no activity against hERG. [1]
In female nude mice bearing C6 tumors, AZD2932 treatment at 3–50 mg/kg b.i.d. 10 h apart give 60–80% inhibition of both p-VEGFR-2 and p-PDGFRb in a 1:1 ratio. [1]
Reference:
1. Plé PA, Jung F, Ashton S, Hennequin L et al. Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases. Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6.
Animal experiment: | Mice: To confirm that AZD2932 has similar potency against both PDGFβ and VEGFR-2 phosphorylation, the female nude mice bearing C6 tumors are dosed iv with VEGF-A and PDGFBB 5 min prior to cull and 6 h post last dose of AZD2932 and the lungs excised immediately after. Lung lysates are analyzed by western blot for total and phosphorylated VEGFR-2 and PDGFβ[1]. |
References: [1]. Plé PA, et al. Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases. Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6. | |
| Cas No. | 883986-34-3 | SDF | |
| 化学名 | (Z)-2-(4-((6,7-dimethoxyquinazolin-4-yl)oxy)phenyl)-N-(1-isopropyl-1H-pyrazol-4-yl)acetimidic acid | ||
| Canonical SMILES | CC(N1C=C(/N=C(O)/CC2=CC=C(OC3=NC=NC4=CC(OC)=C(OC)C=C43)C=C2)C=N1)C | ||
| 分子式 | C24H25N5O4 | 分子量 | 447.49 |
| 溶解度 | DMF: 0.25 mg/ml,DMSO: 0.25 mg/ml | 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 | 2.2347 mL | 11.1734 mL | 22.3469 mL |
| 5 mM | 0.4469 mL | 2.2347 mL | 4.4694 mL |
| 10 mM | 0.2235 mL | 1.1173 mL | 2.2347 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet