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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cdc2-like Kinase (CLK)-Cirtuvivint
Cirtuvivint

Chemical Structure : Cirtuvivint

CAS No.: 2143917-62-6

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Cirtuvivint (SM08502, SM-08502)

货号: PC-72099Not For Human Use, Lab Use Only.

Cirtuvivint (SM08502) is a novel potent, selective inhibitor of CDC-like kinase (CLK) with IC50 of 2/22 nM against CLK2/3.

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10 mg ￥3680 In stock
25 mg ￥5680 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Cirtuvivint (SM08502) is a novel potent, selective inhibitor of CDC-like kinase (CLK) with IC50 of 2/22 nM against CLK2/3.
Cirtuvivint (SM08502) demonstrated 550-fold and 50-fold selectivity for CLK2 and CLK3 inhibitory activity, respectively, compared to CDK1 inhibition (IC50 = 1.1 uM), and good selectivity with 19 of 402 wild-type kinases (4.7%, IC50≤0.05 uM) or within 25-fold of that of CLK2.
Cirtuvivint (SM08502) also shows potential proximal targets included CLK1 (8 nM), CLK4 (1 nM), and the DYRK kinases (DYRK1A/1B, 2-13 nM).
Cirtuvivint (SM08502) strongly inhibited Wnt pathway signaling activity (EC50=46 nM) as assessed with the TOPflash β-catenin/TCF-responsive reporter assay in SW480 colon cancer cells, 10-fold more potent than PRI-724.
Cirtuvivint (SM08502) significantly inhibited Wnt3a-stimulated gene expression (AXIN2, LEF1) in HEK-293T cells; SM08502 inhibited SRSF phosphorylation and expression of Wnt pathway genes, SM08502 induced the generation of splicing variants of Wnt pathway genes.
Cirtuvivint (SM08502) significantly inhibited growth of gastrointestinal tumors and decreased SRSF phosphorylation and Wnt pathway gene expression in xenograft mouse models.

物理化学性质&存储条件

分子量 427.512
分子式 C24H25N7O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-(4-methylpiperazin-1-yl)-N-[6-(1-methyl-1H-pyrazol-4-yl)isoquinolin-3-yl]pyridine-4-carboxamide

参考文献

1. Tam BY, et al. Cancer Lett. 2020 Mar 31;473:186-197.

2. Martín Moyano P, et al. Int J Mol Sci. 2020 Oct 13;21(20):7549.

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