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FMF-04-159-2

Cat. No. 7158 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent covalent CDK14 and CDK16 inhibitor; also inhibits other TAIRE kinase family members
化学名： N-[1-[[3-[[(2E)-4-(Dimethylamino)-1-oxo-2-buten-1-yl]amino]phenyl]sulfonyl]-4-piperidinyl]-4-[(2,4,6- trichlorobenzoyl)amino]-1H-pyrazole-3-carboxamide
纯度： ≥98% (HPLC)
说明书
引用文献
评论
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for FMF-04-159-2

FMF-04-159-2 is a potent inhibitor of CDK14 and CDK16 (IC50 = 40 nM for CDK14 in cellular BRET assay; IC50 values are 88 and 10 nM for CDK14 and CDK16 in kinase activity inhibition assay, respectively). Inhibits other TAIRE kinase family members at 1 μM (CDK17 and CDK18). Also binds CDK2 (IC50 = 256 nM). Displays covalent binding of CDK14, with binding sustained after washout. Causes cell cycle arrest at G2/M in cancer cell lines.

Reversible control FMF-04-159-R (Cat. No. 7159) also available.

许可信息

Sold under license from Dana-Farber Cancer Institute.

化合物库 for FMF-04-159-2

FMF-04-159-2 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。

技术数据 for FMF-04-159-2

分子量 683.01
公式 C28H30Cl3N7O5S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2364489-81-4
InChI Key HZPYSAHDRSBARR-QPJJXVBHSA-N
Smiles CN(C/C=C/C(NC1=CC=CC(S(=O)(N2CCC(NC(C3=NNC=C3NC(C4=C(C=C(C=C4Cl)Cl)Cl)=O)=O)CC2)=O)=C1)=O)C

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for FMF-04-159-2

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 68.3 100
ethanol 13.66 20

制备储备液 for FMF-04-159-2

以下数据基于产品分子量 683.01。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 1.46 mL 7.32 mL 14.64 mL
5 mM 0.29 mL 1.46 mL 2.93 mL
10 mM 0.15 mL 0.73 mL 1.46 mL
50 mM 0.03 mL 0.15 mL 0.29 mL

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参考文献 for FMF-04-159-2

参考文献是支持产品生物活性的出版物。

Ferguson et al (2019) Discovery of covalent CDK14 inhibitors with pan-TAIRE family specificity. Cell Chem.Biol. 26 804 PMID: 30930164

Ferguson et al (2019) Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14 Bioorg.Med.Chem.Letts. 29 1985 PMID: 31175010

If you know of a relevant reference for FMF-04-159-2, please let us know.

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关键词: FMF-04-159-2, FMF-04-159-2 supplier, cyclin, dependent, kinase, Cdk, CDK, inhibitors, inhibits, CDK14, CDK16, CDK2, CDK17, CDK18, TAIRE, family, kinases, covalent, irreversible, CDK5, Subfamily, 7158, Tocris Bioscience

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