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Merck
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文件

SML0569

Sigma-Aldrich

RO-3306

≥98% (HPLC), powder, CDK1 inhibitor

别名:

(5Z)-5-喹啉-6-基甲亚基-2-[(噻吩-2-基甲基)-氨基]-噻唑-4-酮, 5-(6-喹啉基甲亚基)-2-[(2-噻吩基甲基)氨基]-4(5H)-噻唑酮

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About This Item

经验公式（希尔记法）:
C18H13N3OS2
CAS号:
872573-93-8
分子量:
351.45
MDL號碼:
MFCD17392573
分類程式碼代碼:
12352200
PubChem物質ID:
329825559
NACRES:
NA.77

product name

RO-3306, ≥98% (HPLC)

化驗

≥98% (HPLC)

形狀

powder

顏色

off-white to brown

溶解度

DMSO: 5 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

O=C1N=C(NCC2=CC=CS2)S/C1=C\C3=CC4=C(C=C3)N=CC=C4

InChI

1S/C18H13N3OS2/c22-17-16(24-18(21-17)20-11-14-4-2-8-23-14)10-12-5-6-15-13(9-12)3-1-7-19-15/h1-10H,11H2,(H,20,21,22)/b16-10-

InChI 密鑰

XOLMRFUGOINFDQ-YBEGLDIGSA-N

應用

RO-3306已可用于：
  • 研究CA4介导的细胞毒性在有丝分裂阻滞中的重要性
  • 在细胞周期同步化中进行蛋白质组学研究
  • 作为CDK1抑制剂，防止进入早期有丝分裂

生化／生理作用

CDK1（细胞周期蛋白依赖性激酶1）被认为是细胞分裂的“主要开关”，它能够维持细胞的有丝分裂状态。
RO-3306是一种选择性ATP竞争性CDK1抑制剂。 它能够抑制CDK1/cyclin B1的活性，Ki值为35 nM，它对CDK1/cyclin B1的选择性是CDK2/cyclin E的近10倍，是CDK4/cyclin D的50倍以上。RO-3306已可用于使细胞周期阻滞在G2/M期。

特點和優勢

《受体分类和信号转导》手册的 CDK 页面有该化合物的介绍。想要浏览手册的其他页面， 请单击此处。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

分析证书(COA)

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Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1.
Vassilev L T, et al.
Proceedings of the National Academy of Sciences of the USA, 103(28), 10660-10665 (2006)
Tamara B Garcia et al.
Leukemia research, 64, 30-33 (2017-11-28)
Inhibition of WEE1 is emerging as a promising chemosensitization strategy in many cancers including acute leukemia. Our lab and others have demonstrated that a small-molecule inhibitor of WEE1, AZD1775, sensitizes acute leukemia cells to cytarabine; however, a mechanism of combinatorial
BRCA2 suppresses replication stress-induced mitotic and G1 abnormalities through homologous recombination.
Feng W and Jasin M
Nature Communications, 8(1), 525-525 (2017)
Structurally simplified biphenyl combretastatin A4 derivatives retain in vitro anti-cancer activity dependent on mitotic arrest.
Tarade D, et al.
PLoS ONE, 12(3), e0171806-e0171806 (2017)
Visualization of human karyopherin beta-1/importin beta-1 interactions with protein partners in mitotic cells by co-immunoprecipitation and proximity ligation assays.
Francesco L, et al.
Scientific Reports, 8(1), 1850-1850 (2018)
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