KIF18A-IN-2

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

KIF18A-IN-2 

KIF18A-IN-2 是一种有效的 KIF18A 抑制剂 (IC50=28 nM)。KIF18A-IN-2 能引起明显的有丝分裂停滞，增加肿瘤组织中有丝分裂细胞的数量。KIF18A-IN-2 可用于肿瘤研究。

KIF18A-IN-2

KIF18A-IN-2 Chemical Structure

CAS No. : 2600559-20-2

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生物活性

KIF18A-IN-2 is a potent KIF18A inhibitor (IC50=28 nM). KIF18A-IN-2 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-2 can be used for researching cancer[1].

IC50 & Target

IC50: 28 nM (KIF18A)[1]
体内研究
(In Vivo)

KIF18A-IN-2 (compound 23) (100 mg/kg; i.p., single) exhibits a significant and sustained pharmacodynamic response, increasing the number of mitotic cells (pH3 positive cells) in tumor tissues for up to 24 hours[1]. Pharmacokinetic Parameters of KIF18A-IN-2 in female CD-1 mice[1].

IP (100 mg/kg)
Cmax (μM) 12.6
AUC0-24 (μM·h) 147
C24h (μM) 2.9
PPB (fu) 0.007

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice (4-7 weeks; injected with human OVCAR-3 HGSOC cells)[1]
Dosage: 100 mg/kg
Administration: i.p., single
Result: Showed a significant and sustained pharmacodynamic response, increasing the number of mitotic cells (pH3 positive cells) in tumor tissues for up to 24 hours.

分子量

534.69

Formula

C25H34N4O5S2
CAS 号

2600559-20-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Tamayo NA, et al. Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe. J Med Chem. 2022;65(6):4972-4990.

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