Ro-3306
目录号: PL02751 纯度: ≥98%
CAS No. :872573-93-8
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中文名称
Ro-3306
中文别名
2-[[(噻吩-2-基)甲基]氨基]-5-[1-(喹啉-6-基)甲-(Z)-亚基]噻唑-4-酮;RO-3306 抑制剂
英文名称
Ro-3306
英文别名
RO-3306;Ro 3306;5-(quinolin-6-ylmethylidene)-2-(thiophen-2-ylmethylamino)-1,3-thiazol-4-one;(5Z)-5-Quinolin-6-ylmethylene-2-[(thiophen-2-ylmethyl)-amino]-thiazol-4-one;5-(6-Quinolinylmethylene)-2-[(2-thienylmethyl)amino]-4(5H)-thiazolone;RO3306;GTPL10095;HMS3747O05;BCP02123;AK251191;5-[(Quinolin-6-yl)methylidene]-2-{[(thiophen-2-yl)methyl]amino}-1,3-thiazol-4(5H)-one;(5Z)-5-(quinolin-6-ylmethylidene)-2-(thiophen-2-ylmethylamino)-1,3-thiazol-4-one;5-(Quinolin-6-ylmethylidene)-2-(thiophen-2-ylmethylimino)-1,3-thiazolidin-4-one
Cas No.
872573-93-8
分子式
C18H13N3Os2
分子量
351.45
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Ro-3306 是一种有效,选择性的 CDK1 抑制剂,对 CDK1,CDK1/cyclin B1 和 CDK2/cyclin E 的 Ki 值为分别为 20 nM,35 nM 和 340 nM。
生物活性
Ro-3306 is a potent and selective inhibitor of CDK1, with K i s of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.
性状
Solid
IC50 & Target[1][2]
CDK1 20 nM (Ki) CDK1/cyclinB1 35 nM (Ki)
体外研究(In Vitro)
RO-3306 is an ATP-competitive inhibitor, and inhibits CDK1/cyclin A complexes with Ki of 110 nM. RO-3306 blocks the cell cycle in the G2/M phase of human cancer cells. RO-3306 (4 μM) induces apoptosis in cancer cells. RO-3306 (5 μM) induces G2/M-phase cell cycle arrest and apoptosis of AML cells in a time-dependent manner. RO-3306 treatment significantly increases the percentage of Annexin V-positive cells in G1-phase cells without affecting the cell cycle distribution. RO-3306 enhances p53-mediated apoptosis. RO-3306 cooperates with Nutlin-3 in activating Bax and inducing mitochondrial apoptosis. RO-3306 (5 μM) downregulates antiapoptotic p21, Bcl-2 and survivin protein expression in AML. RO-3306 inhibits p53-induced p21 synthesis. RO-3306 does not inhibit RNA polymerase II CTD phosphorylation. RO-3306 (10 μM) effectively arrests oocyte maturation. RO-3306 reduces
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]. Vassilev LT, et al. Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1. Proc Natl Acad Sci U S A. 2006 Jul 11;103(28):10660-5.
[2]. Kojima K, et al. Cyclin-dependent kinase 1 inhibitor RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis in AML. Cancer Sci. 2009 Jun;100(6):1128-36.
溶解度数据
In Vitro: DMSO : 25 mg/mL (71.13 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

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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