AZD1152Aurora B kinase inhibitor,highly potent and selective |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MS (Mass Spectrometry)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
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Chemical structure
Related Biological Data
Cell experiment [1]: | |
Cell lines | Leukemia cells from patients, bone marrow mononuclear cellsfrom healthy volunteers |
Preparation method | The solubility of this compound in DMSO is >5.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 1-100 nM |
Applications | AZD1152-HQPA (1-100 nM) induced growth arrest of a variety of types of leukemia cells with the IC50s of approximately 5, 12, and 8 nM for Philadelphia chromosome–positive ALL PALL-2, acute monocytic leukemia MOLM13, and biphenotypic leukemia MV4-11 cells, respectively. AZD1152 (3 μM, 3 hours) significantly decreased expression of the phosphorylated forms of histone H3 in freshly isolated leukemia cells. AZD1152 increased cell 4N/8N DNA content in a dose- and time-dependent manner in MOLM13 and PALL2 cells. AZD1152-HQPA treatment (1-10 nM) for 24 or 48 hours induced apoptosis in a dose-dependent manner. |
Animal experiment [2]: | |
Animal models | Female immune-deficient BALB/c nude mice xenografted with human MOLM13 cells |
Dosage form | 5 or 25 mg/kg, Intraperitoneal injection, 4 times a week or every another day, |
Application | AZD1152 (25 mg/kg) markedly suppressed the growth and weights of AZD1152-treated tumors. |
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] Yang J, Ikezoe T, Nishioka C, et al. AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo[J]. Blood, 2007, 110(6): 2034-2040. [2] Lee TX1, Packer MD, Huang J, Akhmametyeva EM, Kulp SK, Chen CS, Giovannini M, Jacob A, Welling DB, Chang LS.Growth inhibitory and anti-tumour activities of OSU-03012, a novel PDK-1 inhibitor, on vestibular schwannoma and malignant schwannoma cells. Eur J Cancer. 2009 Jun;45(9):1709-20. |
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Cas No. | 722543-31-9 | SDF | Download SDF |
Synonyms | AZD-1152;AZD 1152 | ||
Chemical Name | 2-[ethyl-[3-[4-[[5-[2-(3-fluoroanilino)-2-oxoethyl]-1H-pyrazol-3-yl]amino]quinazolin-7-yl]oxypropyl]amino]ethyl dihydrogen phosphate | ||
Canonical SMILES | CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCOP(=O)(O)O | ||
Formula | C26H31FN7O6P | M.Wt | 587.54 |
Solubility | ≥5.88 mg/mL in DMSO, <2.46 mg/ml="" in="" etoh,="">2.46><2.25 mg/ml="" in="" h2o="">2.25> | Storage | Store at -20°C |
Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
AZD1152 is a highly selective inhibitor of Aurora kinases with IC50 values of 1.37 μM and 0.37 nM for Aurora A and Aurora B, respectively [1].AZD1152 is a dihydrogen phosphate pro-drug of HQPA which is a highly potent and specific inhibitor of the serine/threonine kinase Aurora kinases. The expression of Aurora kinase A and B are found to be related with the development of various cancers such as ovarian, pancreatic, breast and colon. Since that, the Aurora family is regarded as attractive target for anticancer treatment. As a selective Aurora kinase inhibitor, AZD1152 showed no significant effect on other kinases including JAK2, FLT3 and Abl. Besides that, AZD1152 exerted potent antitumor activities through inhibiting tumor cell proliferation and inducing apoptosis [1]. AZD1152 treatment potently inhibited cell growth in various leukemic cells including ALL PALL-2, MV4-11 and MOLM13 with IC50 values of 5, 1and 2.8 nM, respectively. AZD1152 also inhibited clone formation of freshly isolated leukemia cells with IC50 values of less than 3 nM. For the colon cancer HCT-116 cells, incubation of AZD1152 at dose of 30 nM for one day resulted in 80% cell number reduction after 4 days drug wash out. In prostate cancer DU145 and PC3 cells, AZD1152 caused decrease of G0/G1-phase cells and induced G2/M cell cycle arrest. Moreover, AZD1152 treatment enhanced the radio sensitivity of prostate cancer cells which were androgen-insensitive [1, 2 and 3].In mice model with human MOLM13 cell xenografts, administration of AZD1152 at dose of 25 mg/kg significantly inhibited tumor growth. The combination treatment of AZD1152 at dose of 5 mg/kg and vincristine at dose of 0.2 mg/kg resulted in almost 100% inhibition of tumor growth of MOLM13 xenografts. In mice injected with MiaPaCa-2cells, the combination of AZD1152 and gemcitabine showed more than double effective than the single treatment [1 and 2]. References:[1] Yang J, Ikezoe T, Nishioka C, Tasaka T, Taniguchi A, Kuwayama Y, Komatsu N, Bandobashi K, Togitani K, Koeffler HP, Taguchi H, Yokoyama A. AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo. Blood. 2007 Sep 15;110(6):2034-40. [2] Azzariti A, Bocci G, Porcelli L, Fioravanti A, Sini P, Simone GM, Quatrale AE, Chiarappa P, Mangia A, Sebastian S, Del Bufalo D, Del Tacca M, Paradiso A. Aurora B kinase inhibitor AZD1152: determinants of action and ability to enhance chemotherapeutics effectiveness in pancreatic and colon cancer. Br J Cancer. 2011 Mar 1;104(5):769-80. [3] Niermann KJ, Moretti L, Giacalone NJ, Sun Y, Schleicher SM, Kopsombut P, Mitchell LR, Kim KW, Lu B. Enhanced radiosensitivity of androgen-resistant prostate cancer: AZD1152-mediated Aurora kinase B inhibition. Radiat Res. 2011 Apr;175(4):444-51.
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1. Buffer中离子浓度过大,甘氨酸或者Tris碱有可能疏忽多加了
2.没有加相应浓度的SDS
3.电泳周围温度高,也是一个原因
此外,我们常常用“电泳法”判断液体的性质,是胶体还是溶液。在高中化学中我们就用过这种方法判断给定的液体是否为胶体。向左转|向右转
TAE是使用最广泛的缓冲系统。其特点是超螺旋在其中电泳时更符合实际相对分子质量(TBE中电泳时测出的相对分子质量会大于实际分子质量),且双链线状DNA在其中的迁移率较其他两种缓冲液快约10%,电泳大于13kb的片段时用TAE缓冲液将取得更好的分离效果,此外,回收DNA片段时也易用TAE缓冲系统进行电泳。TAE的缺点是缓冲容量小,长时间电泳(如过夜)不可选用,除非有循环装置使两极的缓冲液得到交换。 50×TAE Buffer 配制方法: 1. 称量Tris 242g,Na2EDTA.2H2O 37.2g 于1L烧杯中; 2.向烧杯中加入约800ml去离子水,充分搅拌均匀; 3加入57.1ml的冰乙酸,充分溶解; 4.加去离子水定容至1L后,室温保存。向左转|向右转
加样缓冲液的主要作用是使PCR产物与其混合,使DNA沉于加样孔的底部,防止DNA跑出来.
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