规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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体外研究 (In Vitro) |
在新分离的白血病细胞中,barasertib-HQPA(3 μM,3 小时)可显着降低组蛋白 H3 磷酸化变体的表达 [1]。在血浆中,barasertib-HQPA 快速转化为活性 barasertib-HQPA [2]。在 LNCaP 细胞系中,barasertib-HQPA 治疗会导致细胞存活不佳、多倍体和细胞死亡 [3]。 barasertib-HQPA 引起的显着抗增殖作用伴随着多倍体群体的出现,这通常会导致细胞凋亡[4]。
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体内研究 (In Vivo) |
barasertib-HQPA(AZD1152,25 mg/kg)显着降低了接受 AZD1152 治疗的肿瘤的发育和重量[1]。在人 MOLM13 白血病异种移植物中,barasertib-HQPA(AZD1152,5 mg/kg)可增强长春新碱或柔红霉素引起的增殖抑制作用[1]。 barasertib-HQPA(AZD1152,10–150 mg/kg/d)可有效抑制免疫缺陷小鼠体内的人类结肠、肺和血液肿瘤异种移植物(平均肿瘤生长抑制范围,55% 至 z100%;P < 0.05)[2] 。
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细胞实验 |
细胞增殖测定[1]。
细胞类型: AML 系(HL-60、NB4、MOLM13)、ALL 系(PALL-2)、双表型白血病(MV4-11)、急性嗜酸性粒细胞白血病(EOL-1)、以及慢性粒细胞白血病K562细胞的急变。 测试浓度:0-100 nM。 (Barasertib -HQPA) 孵育时间: 48 小时。 实验结果:IC50值范围为3 nM至40 nM。 |
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动物实验 |
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参考文献 |
[1]. Yang, Jing., 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. Blood. 2007 Sep 15;110(6):2034-40.
[2]. Wilkinson RW, et al. AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis. Clin Cancer Res. 2007 Jun 15;13(12):3682-8. [3]. Zekri A, et al. AZD1152-HQPA induces growth arrest and apoptosis in androgen-dependent prostate cancer cell line (LNCaP) via producing aneugenic micronuclei and polyploidy. Tumour Biol. 2015 Feb;36(2):623-32. [4]. Oke A, et al. AZD1152 rapidly and negatively affects the growth and survival of human acute myeloid leukemia cells in vitro and in vivo. Cancer Res. 2009 May 15;69(10):4150-8. |
分子式 |
C26H30FN7O3
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分子量 |
507.56
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CAS号 |
722544-51-6
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相关CAS号 |
Barasertib;722543-31-9
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SMILES |
O=C(NC1=CC=CC(F)=C1)CC2=CC(NC3=C4C=CC(OCCCN(CC)CCO)=CC4=NC=N3)=NN2
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InChi Key |
QYZOGCMHVIGURT-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C26H30FN7O3/c1-2-34(10-11-35)9-4-12-37-21-7-8-22-23(16-21)28-17-29-26(22)31-24-14-20(32-33-24)15-25(36)30-19-6-3-5-18(27)13-19/h3,5-8,13-14,16-17,35H,2,4,9-12,15H2,1H3,(H,30,36)(H2,28,29,31,32,33)
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化学名 |
2-(3-((7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-yl)amino)-1H-pyrazol-5-yl)-N-(3-fluorophenyl)acetamide
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别名 |
INH-34; INH34; AZD 2811; AZD2811; INH 34; AZD1152-HQPA; AZD1152; AZD-1152; AZD 1152 HQPA; AZD-2811; AZD-1152HQPA; AZD 1152HQPA; AZD1152HQPA; AZD1152 HQPA; AZD1152-HQPA; AZD1152HQPA.
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% propylene glycol:30mg/mL 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9702 mL | 9.8511 mL | 19.7021 mL | |
5 mM | 0.3940 mL | 1.9702 mL | 3.9404 mL | |
10 mM | 0.1970 mL | 0.9851 mL | 1.9702 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01019161 | Completed | Drug: AZD1152 Drug: C14 AZD1152 |
Acute Myeloid Leukaemia | AstraZeneca | November 2009 | Phase 1 |
NCT03217838 | Terminated | Drug: AZD2811 Drug: Azacitidine |
Acute Myeloid Leukaemia | AstraZeneca | July 31, 2017 | Phase 1 |
NCT00926731 | Completed | Drug: AZD1152 Drug: LDAC (low dose cytosine arabinoside) |
Acute Myeloid Leukemia | AstraZeneca | June 2009 | Phase 1 |