IQTub4P

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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。

IQTub4P 

IQTub4P 是一种有效的微管 (microtubule ) 抑制剂。IQTub4P 在 HeLa 细胞中具有细胞毒性，其 EC50 为 170 nM。IQTub4P 抑制微管结构和功能。IQTub4P 在体内时耐受良好。

IQTub4P

IQTub4P Chemical Structure

CAS No. : 2376321-67-2

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生物活性

IQTub4P is a potent microtubule (MT) inhibitor. IQTub4P has the cytotoxicity in in HeLa cells, with EC50 of 170 nM. IQTub4P inhibits microtubule structure and function. IQTub4P is well-tolerated in vivo[1].

体外研究
(In Vitro)

IQTub4P (48 h) shows strong dose-dependent cytotoxicity in HeLa cells[1].
IQTub4P (0-750 nM, 15 min) shows dose-dependent microtubule network depolymerisation, leads to mitotic arrests and the formation of aberrant multipolar spindles with resulting unstructured chromosome alignment at 120 nM[1].
IQTub4P (0-1.25 μM, 24 h) shows potent induction of G2/M arrest[1].
IQTub4P (10 μM, 2 min) shows potent inhibition of cellular tubulin polymerisation dynamics[1].

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

Cell Viability Assay

Cell Line: HeLa cells[1]
Concentration:
Incubation Time: 48 h
Result: Showed strong dose-dependent cytotoxicity in HeLa cells, with EC50 of 170 nM, and displayed near-identical cytotoxicity in cell culture as its free phenol form IQTub4 (EC50 = 120 nM).

Cell Cycle Analysis

Cell Line: HeLa cells[1]
Concentration: 0, 0.06, 0.12, 0.5, 0.75, 1.25 μM
Incubation Time: 24 h
Result: Showed potent induction of G2/M arrest, and showed extensive G2/M-arrest from 500 nM.

体内研究
(In Vivo)

IQTub4P (Balb/c mice, 25 mg/kg, IP and IV, once every two days, 3 administrations) is well-tolerated in vivo and can avoid short-term cumulative toxicity[1].

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

Animal Model: Balb/c mice (female)[1]
Dosage: 25 mg/kg
Administration: IP and IV, 3 administration, 48 h intervals
Result: Could avoid short-term cumulative toxicity, and was well-tolerated in vivo, with a single-administration maximal tolerated dose of 32 mg/kg (i.p.) and 50 mg/kg (i.v.).

分子量

465.30

Formula

C19H18NNa2O8P
CAS 号

2376321-67-2
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]. Kraus Y, Glas C, Melzer B, et al. Isoquinoline-based biaryls as a robust scaffold for microtubule inhibitors. Eur J Med Chem. 2020;186:111865.

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