文献支持CCT 137690是有效的，有口服活性的极光激酶 (aurora) 抑制剂，对极光激酶A，B，C的 IC50 值分别为15，25 和19 nM。

价格： ￥358

品牌：medchemexpress(MCE)

货号：HY-10804

产品详情

CCT 137690

CCT 137690是有效的，有口服活性的极光激酶 (aurora) 抑制剂，对极光激酶A，B，C的 IC₅₀ 值分别为15，25 和19 nM。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物，拥有着多年的发展历程和丰富的行业经验。从产品的HNMR数据解析到生物活性数据，从客户的询价到产品的售后服务，我们拥有着完善的管理体系，从而保证我们的服务更加高效、准确。努力为中国的医药行业发展注入新的活力，我们将成为您研发工作值得信赖的伙伴。

生物活性
CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively.

体外研究
CCT 137690 displays antiproliferative activity in a range of human tumor cell lines, including SW620 colon carcinoma (GI50=0.30 μM) and A2780 ovarian cancer cell line (GI50=0.14 μM). CCT 137690 inhibits in vitro phosphorylation of histone H3. CCT 137690 is a moderate inhibitor of the hERG ion-channel (IC50=3.0 μM)[1]. CCT137690 efficiently inhibits histone H3 and TACC3 phosphorylation (Aurora B and Aurora A substrates, respectively) in HCT116 and HeLa cells. Continuous exposure of tumour cells to the inhibitor causes multipolar spindle formation, chromosome misalignment, polyploidy and apoptosis[2].

体内研究
CCT 137690 slows the growth of the SW620 xenografts with no observed toxicity[1]. CCT 137690 significantly inhibits tumour growth in a transgenic mouse model of neuroblastoma (TH-MYCN) that overexpresses MYCN protein and is predisposed to spontaneous neuroblastoma formation[2].

分子量
551.48

性状
Solid

Formula
C26H31BrN8O

CAS 号
1095382-05-0

运输条件
Room temperature in continental US; may vary elsewhere.

储存方式
Powder   -20°C   3 years
4°C   2 years
In solvent   -80°C   6 months
-20°C   1 month
溶解性数据
In Vitro:
DMSO : 16.67 mg/mL (30.23 mM; Need ultrasonic)

配制储备液
浓度溶剂体积质量   1 mg   5 mg   10 mg
1 mM   1.8133 mL   9.0665 mL   18.1330 mL
5 mM   0.3627 mL   1.8133 mL   3.6266 mL
10 mM   0.1813 mL   0.9067 mL   1.8133 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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: ≥ 1.67 mg/mL (3.03 mM); Clear solution

2.
请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.67 mg/mL (3.03 mM); Clear solution

3.
请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 1.67 mg/mL (3.03 mM); Clear solution

参考文献	[1]. Bavetsias V, et al. Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. J Med Chem. 2010 Jul 22;53(14):5213-28. [Content Brief] [2]. Faisal A, et al. The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Mol Cancer Ther. 2011 Nov;10(11):2115-23. [Content Brief]

参考文献

[1]. Bavetsias V, et al. Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. J Med Chem. 2010 Jul 22;53(14):5213-28. [Content Brief]

[2]. Faisal A, et al. The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Mol Cancer Ther. 2011 Nov;10(11):2115-23. [Content Brief]

参考文献	[1]. Bavetsias V, et al. Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. J Med Chem. 2010 Jul 22;53(14):5213-28. [Content Brief] [2]. Faisal A, et al. The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Mol Cancer Ther. 2011 Nov;10(11):2115-23. [Content Brief]