CCT 137690|1095382-05-0|-陌孚医药/Medlife

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CCT 137690

目录号: PL13943 纯度: ≥99%

CAS No. :1095382-05-0

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中文名称	CCT 137690
中文别名	3-((4-(6-溴-2-(4-(4-甲基哌嗪-1-基)苯基)-3H-咪唑并[4,5-b]吡啶-7-基)哌嗪-1-基)甲基)-5-甲基异噁唑;3-[[4-[6-溴-2-[4-(4-甲基哌嗪-1-基) 苯基]-3H-咪唑并[4,5-b]吡啶-7-基]哌嗪-1-基]甲基]-5-甲基异恶唑;CCT137690 抑制剂;3-[[4-[6-溴-2-[4-(4-甲基哌嗪-1-基)苯基]-3H-咪唑并[4,5-b]吡啶-7-基]哌嗪-1-基]甲基]-5-甲基异恶唑;3-((4-(6-溴-2-(4-(4-甲基哌嗪-1-基)苯基)-3H-咪唑并[4,5-b]吡啶-7-基)哌嗪-1-基)甲基)-5-甲基异恶唑
英文名称	CCT 137690
英文别名	CCT137690;3-[[4-[6-bromo-2-[4-(4-methylpiperazin-1-yl)phenyl]-1H-imidazo[4,5-b]pyridin-7-yl]piperazin-1-yl]methyl]-5-methyl-1,2-oxazole;CCT-137690;3-((4-(6-bromo-2-(4-(4-methylpiperazin-1-yl)phenyl)-3H-imidazo[4,5-b]pyridin-7-yl)piperazin-1-yl)methyl)-5-methylisoxazole;3-((4-(6-bromo-2-(4-(4-methylpiperazin-1-yl)phenyl)-3H-imidazo-[4,5-b]pyridin-7-yl)piperazin-1-yl)methyl)-5-methylisoxazole;BCP9000498;cc-66;CHEBI:799254;CHEMBL1236904;CS-0706;SureCN4755249;6-Bromo-7-[4-[(5-methyl-3-isoxazolyl)methyl]-1-piperazinyl]-2-[4-(4-methyl-1-piperazinyl)phenyl]-3H-imidazo[4,5-b]pyridine;3-[[4-[6-Bromo-2-[4-(4-methylpiperazin-1-yl)phenyl]-3H-imidazo[4,5-b]pyridin-7-yl]piperazin-1-yl]methyl]-5-methylisoxazole;CCT 137690
Cas No.	1095382-05-0
分子式	C₂₆H₃₁N₈OBr
分子量	551.48
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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。
生物活性	CCT 137690 is a potent and orally available aurora kinase inhibitor with IC 50 s of 15, 25, and 19 nM for aurora A, B and C, respectively.
性状	Solid
IC50 & Target[1][2]	Aurora A 15 nM (IC50) Aurora B 25 nM (IC
体外研究(In Vitro)	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). 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	CCT 137690 slows the growth of the SW620 xenografts with no observed toxicity. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
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
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. [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.

溶解度数据	In Vitro: DMSO : 16.67 mg/mL (30.23 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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