| 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)
- Datasheet
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,=""><2.25 mg/ml="" in="" h2o=""> | 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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② 应取pH8.0，这样可使核苷酸带较多负电荷，利于吸附于阴离子交换树脂柱。虽然pH 11.4时核苷酸带有更多的负电荷，但pH过高对分离不利。
③ 当不考虑树脂的非极性吸附时，根据核苷酸负电荷的多少来决定洗脱速度，则洗脱顺序为CMP>AMP> GMP > UMP，但实际上核苷酸和聚苯乙烯阴离子交换树脂之间存在着非极性吸附，嘌呤碱基的非极性吸附是嘧啶碱基的3倍。静电吸附与非极性吸附共同作用的结果使洗脱顺序为：CMP> AMP > UMP >GMP。
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
我使用的是1%琼脂糖凝胶，电泳缓冲液为0.5×TBE。
请问各位大虾，在不影响实验结果的前提下，这样的含EB的电泳缓冲液可以反复使用多少次？
谢谢^_^
500ml
2。阴极缓冲液 ( 10 × ) ：将 60.55g Tris ,89.58g Tricine 及 5g SDS 溶于400ml 蒸馏水中，加水至终体积为500ml
使用时稀释至1×的缓冲液，电泳槽内槽加入阴极电泳缓冲液，外槽加入阳极电泳缓冲液。形成Trcine-SDS-PAGE电泳系统。
如果你是制胶或者做电泳缓冲液的话，不用灭菌。
Tris-Glycine/SDS;
MOPS/SDS;
Bis-Glycine/SDS等不同的缓冲液、预混液等。
不知道这几种缓冲液有什么异同呢？
比如如果是Invitrogen的预制胶-预混液电泳系统，每种预制胶有适配缓冲液，但是如果用其他的缓冲液似乎也可以得到不错的结果，那么是否说明电泳缓冲液只要满足了缓冲ph范围，其他的不是特别重要呢？
此外，附加提问是，PVDF膜在转膜的时候，转膜缓冲液中不需要加入甲醇，那么是加入甲醇转膜效果好还是不加好呢？
谢谢！
