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LDC 000067

Cat. No. 6752 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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Cat.No. 6752 - LDC 000067 | C18H18N4O3S | CAS No. 1073485-20-7
说明： Potent and selective CDK9 inhibitor
化学名： 3-[[6-(2-Methoxyphenyl)-4-pyrimidinyl]amino]benzenemethanesulfonamide
纯度： ≥98% (HPLC)
说明书
引用文献
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文献
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

Potent and selective CDK9 inhibitor (IC50 = 44 nM at CDK9-cyclin T1). Inhibits other CDKs in the micromolar range (IC50 values are 2.4, 5.5, 9.2, >10 and >10 μM for CDK2-cyclin A, CDK1-cyclin B1, CDK4-cyclin D1, CDK6-cyclin D3 and CDK7-cyclin H-MAT1, respectively). Inhibits P-TEFb-dependent in vitro transcription. Induces apoptosis in vitro and in vivo in combination with BI 894999.

技术数据

分子量 370.43
公式 C18H18N4O3S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1073485-20-7
PubChem ID 25104564
InChI Key GGQCIOOSELPMBB-UHFFFAOYSA-N
Smiles COC1=C(C2=NC=NC(NC3=CC(CS(N)(=O)=O)=CC=C3)=C2)C=CC=C1

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

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 37.04 100

制备储备液

以下数据基于产品分子量 370.43。 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.

浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.7 mL 13.5 mL 27 mL
5 mM 0.54 mL 2.7 mL 5.4 mL
10 mM 0.27 mL 1.35 mL 2.7 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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参考文献

参考文献是支持产品生物活性的出版物。

Albert et al (2014) Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor. Br.J.Pharmacol. 171 55 PMID: 24102143

Gerlach et al (2018) The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML. Oncogene 37 2687 PMID: 29491412

Brägelmann et al (2017) Systematic kinase inhibitor profiling identifies CDK9 as a synthetic lethal target in NUT midline carcinoma. Cell Rep. 20 2833 PMID: 28930680

Jorda et al (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 61 9105 PMID: 30234987

If you know of a relevant reference for LDC 000067, please let us know.

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关键词: LDC 000067, LDC 000067 supplier, LDC000067, LDC67, LDC067, potent, selective, CDK9, inhibitors, inhibits, Cyclin-dependent, Kinase, 6752, Tocris Bioscience

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