CD532 是一种有效的Aurora A激酶抑制剂，IC50值为 45 nM。CD532 具有阻断 Aurora A 激酶活性和驱动 MYCN 降解的双重作用。CD532 还可以直接与 AURKA 相互作用并诱导整体构象转变。CD532 可用于癌症的研究。
| 生物活性 | CD532 is a potentAurora Akinaseinhibitor with anIC50of 45 nM. CD532 has the dual effect of blockingAurora Akinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research ofcancer[1][2]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | CD532 (1-10000 nM; 72 h) is cytotoxic in MYCN-amplified neuroblastoma cell lines SK-N-BE(2) and Kelly, with EC50s of 223.2 nM and 146.7 nM, respectively[1].
CD532 (0.1-1 μM; 24 h) causes dose-dependent loss of MYCN protein in SK-N-BE(2) cells[1].
CD532 (1 μM; 6 h) prevents S-phase entry in SK-N-BE(2) cells[1].
Cell Viability Assay[1] | Cell Line: | SK-N-BE(2) and Kelly cells | | Concentration: | 1, 10, 100, 1000, 10000 nM | | Incubation Time: | 72 hours | | Result: | Inhibited the cell viability of SK-N-BE(2) and Kelly cells, with EC50s of 223.2 nM and 146.7 nM, respectively. |
Cell Cycle Analysis[1] | Cell Line: | SK-N-BE(2) cells | | Concentration: | 1 μM | | Incubation Time: | 4 hours | | Result: | Resulted in a rapid and potent loss of S-phase and accumulation in both G0/G1 and G2. |
Western Blot Analysis[1] | Cell Line: | SK-N-BE(2) cells | | Concentration: | 0.1, 0.25, 0.5, 1 μM | | Incubation Time: | 2, 4, 6, 24 hours | | Result: | Causes dose-dependent and time-dependent loss of MYCN protein. |
|
体内研究
(In Vivo) | CD532 (25 mg/kg; i.p. twice weekly for 3 weeks) decreases the tumor volume and increases survival in mice with subcutaneous sonic hedgehog (SHH)-subtype medulloblastoma[1].
CD532 (60 mg/kg; i.p. for 2 days) decreases the level of MYCN protein in MYCN-amplified neuroblastoma xenografts[1].
CD532 (20 mg/kg; i.p.) shows a serum half-life of ~1.5 hours and AUC0-24 of 27 μMoh in mice[1].
| Animal Model: | Homozygous nu/nu mice with SHH-subtype MYCN-expressing medulloblastoma[1] | | Dosage: | 25 mg/kg | | Administration: | I.p. twice weekly for 3 weeks | | Result: | Decreased the level of MYCN protein and tumor volume and increases survival. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(478.45 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9138 mL | 9.5690 mL | 19.1380 mL | | 5 mM | 0.3828 mL | 1.9138 mL | 3.8276 mL | | 10 mM | 0.1914 mL | 0.9569 mL | 1.9138 mL |
In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (3.98 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.98 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (3.98 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.98 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (3.98 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.98 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
m.cnreagent.com