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AZD 6482
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产品介绍
产品介绍
产品信息
简单描述
AZD 6482 is a PI3K inhibitor that targets the β isoform more potently than PI3Kδ, PI3Kγ, or PI3Kα (IC50s = 0.69, 13.6, 47.8, and 136 nM, respectively).1 It displays 80-fold selectivity for PI3Kβ over PI3k-C2 and DNA-PK and more than 1,000-fold over other PI3K-related kinases.1 AZD 6482 blocks Akt signaling and tumor growth in a large number of cancer cell lines, including those that are dependent on PI3Kβ activation or PTEN loss.1,2,3 AZD 6482 (20 mg/kg, i.p.) suppresses the growth of PTEN-deficient xenograft tumors in mice.1 It also produces an anti-thrombotic effect in dogs without an increase in bleeding time or blood loss.4WARNING This product is not for human or veterinary use.
商品描述
A PI3Kβ inhibitor
分子量
408.5
纯度
≥98%
产品类型
Biochemicals/Kinase Inhibitors/PI3K/Small Molecule Inhibitors/Kinases
背景
别名
Formal_Name:2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]-benzoic acid;Synonyms:KIN-193
研究领域
Cancer/Cell Signaling/PI3K/Akt/mTOR Signaling,Cardiovascular System/Blood/Thrombosis
结构式
O=C1N2C(C([C@@H](C)NC3=C(C(O)=O)C=CC=C3)=CC(C)=C2)=NC(N4CCOCC4)=C1
分子式
C22H24N4O4
CAS号
1173900-33-8
制备和贮存
保存
≥ 4 years
溶解方法
DMF: 10 mg/ml
DMSO: 10 mg/ml
Ethanol: 5 mg/ml
保存方式
-20°C
文献
文献
1.Rameh, L.E. and Cantley, L.C. The role of phosphoinositide 3-kinase lipid products in cell function. The Journal of Biological Chemisty 274, 8347-8350 (1999).
2.Vivanco, I. and Sawyers, C.L. The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nature Reviews.Cancer 2, 489-501 (2002).
3.Hennessy, B.T.,Smith, D.L.,Ram, P.T., et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nature Reviews.Drug Discovery 4, 988-1004 (2005).
4.Rückle, T.,Schwarz, M.K. and Rommel, C. PI3Kγ inhibition: Towards an 'aspirin of the 21st century'? Nature Reviews.Drug Discovery 5, 903-918 (2006).
5.Ni, J.,Liu, Q.,Xie, S., et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2(5), 425-433 (2012).
6.Weigelt, B.,Warne, P.H.,Lambros, M.B., et al. PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clinical Cancer Research 19(13), 3533-3544 (2013).
7.Nichols, A.C.,Black, M.,Yoo, J., et al. Exploiting high-throughput cell line drug screening studies to identify candidate therapeutic agents in head and neck cancer. BMC Pharmacol.Toxicol. 15, (2014).
8.Nylander, S.,Kull, B.,Björkman, J.A., et al. Human target validation of phosphoinositide 3-kinase (PI3K)β: Effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor. J.Thromb.Haemost. 10(10), 2127-2136 (2012).
2.Vivanco, I. and Sawyers, C.L. The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nature Reviews.Cancer 2, 489-501 (2002).
3.Hennessy, B.T.,Smith, D.L.,Ram, P.T., et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nature Reviews.Drug Discovery 4, 988-1004 (2005).
4.Rückle, T.,Schwarz, M.K. and Rommel, C. PI3Kγ inhibition: Towards an 'aspirin of the 21st century'? Nature Reviews.Drug Discovery 5, 903-918 (2006).
5.Ni, J.,Liu, Q.,Xie, S., et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2(5), 425-433 (2012).
6.Weigelt, B.,Warne, P.H.,Lambros, M.B., et al. PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clinical Cancer Research 19(13), 3533-3544 (2013).
7.Nichols, A.C.,Black, M.,Yoo, J., et al. Exploiting high-throughput cell line drug screening studies to identify candidate therapeutic agents in head and neck cancer. BMC Pharmacol.Toxicol. 15, (2014).
8.Nylander, S.,Kull, B.,Björkman, J.A., et al. Human target validation of phosphoinositide 3-kinase (PI3K)β: Effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor. J.Thromb.Haemost. 10(10), 2127-2136 (2012).
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