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My CartCAS：883986-34-3
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 883986-34-3 |
| Name | AZD-2932 |
| Molecular Formula | C24H25N5O4 |
| Molecular Weight | 447.49 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD25977021 |
| SMILES | O=C(NC1=CN(C(C)C)N=C1)CC2=CC=C(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)C=C2 |
| Target Point | VEGFR-2;PDGFRβ;Flt-3;c-Kit |
| Passage | Angiogenesis; Protein Tyrosine Kinase/RTK |
| Background | It is a potent multi-targeted kinase inhibitor. |
| Biological Activity | AZD2932是有效的多靶点激酶抑制剂，细胞试验中的抑制VEGFR2，PDGFβ，PDGFβ 和 PDGFβ 的 IC50 值分别为8，4，7，9 nM。[1] |
| IC50 | VEGFR2:8nM;PDGFRβ:4nM;FLT3:7nM;c-Kit:9nM[1] |
| In Vitro | AZD2932具有针对PDGFβ，VEGFR-2，Flt-3和c-Kit的有效且平衡的特征。它不抑制各种细胞色素P450同种型，最差的IC50与2C9(8.0μM)相比。 AZD2932对hERG没有活性(IC50 =137μM)[1]。 |
| In Vivo | 每天两次口服给药(bid)AZD2932 10小时导致对照动物终止当天50和12.5mg / kg剂量的显著肿瘤生长抑制为64％。携带非PDGFβ表达肿瘤细胞的异种移植物也对AZD2932治疗敏感：Calu-6肿瘤的生长在50和12.5mg / kg bid下被抑制81％和72％，并且LoVo肿瘤在50mg / kg bid下被抑制67％。是由于AZFR2932对VEGFR2的有效活性以及由于PDGFR a和b抑制对周细胞和肿瘤相关成纤维细胞的潜在影响。 AZD2932以3-50mg / kg bid间隔10小时，以1：1的比例对p-VEGFR2和p-PDGFβ进行60-80％的抑制[1]。 |
| Animal Experiment | 小鼠：为了证实AZD2932对PDGFβ和VEGFR-2磷酸化具有相似的效力，携带C6肿瘤的雌性裸鼠在剔除前5分钟和最后一剂AZD2932和肺部后6小时静脉注射VEGF-A和PDGFBB。之后立即切除。通过蛋白质印迹分析肺裂解物的总和磷酸化VEGFR-2和PDGFβ[1]。 |
| Data Literature Source | [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. |
| Unit | Bottle |
| Specification | 2mg 5mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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