ATX inhibitor 13

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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。

ATX inhibitor 13 

ATX inhibitor 13 (compound 10c) 是一种口服有效的 ATX 抑制剂，其IC50 为 3.4 nM。ATX inhibitor 13 抑制 RAW264.7 细胞的增殖和迁移，诱导细胞凋亡和 G2 期阻滞。ATX inhibitor 13 抑制肿瘤细胞集落形成。

ATX inhibitor 13

ATX inhibitor 13 Chemical Structure

CAS No. : 2485779-34-6

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生物活性

ATX inhibitor 13 (10c) is an orally active and potent ATX inhibitor, with an IC50 of 3.4 nM. ATX inhibitor 13 inhibits proliferation and migration, and induces apoptosis and G2 phase arrest in RAW264.7 cells. ATX inhibitor 13 suppresses tumor cell colony formation[1].

IC50 & Target

ATX

3.4 nM (IC50)

体外研究
(In Vitro)

ATX inhibitor 13 (compound 10c) (0-20 μM, 72 h) shows cytotoxicity and anti-proliferative activity against MCF-7, MDA-MB-231, A549, NCI-H1581, H2228, Hep3B, and RAW264.7 cells[1].
ATX inhibitor 13 (0-1 μM, 0-72 h) inhibits migration of RAW264.7 cells in a dose-dependent manner, significantly down-regulates both the colony count and colony single area with the concentration elevation[1].
ATX inhibitor 13 (0-1 μM, 72 h) dose dependently suppresses colony formation of RAW264.7 cells[1].
ATX inhibitor 13 (0-1 μM, 48 h) induces weak apoptosis in a dose-dependent manner in RAW264.7 cells[1].
ATX inhibitor 13 (0-1 μM, 48 h) brings G2 phase arrest of RAW264.7 cells[1].

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

Cell Proliferation Assay

Cell Line: MCF-7, MDA-MB-231, A549, NCI-H1581, H2228, Hep3B, RAW264.7[1]
Concentration: 0-20 μM
Incubation Time: 72 h
Result: Showed cytotoxicity and antiproliferative activity against MCF-7, MDA-MB-231, A549, NCI-H1581, H2228, Hep3B, and RAW264.7 cell lines, with IC50 values of 3.87 ± 0.37, 3.29 ± 0.37, 6.59 ± 0.26, 4.76 ± 0.57, 4.27 ± 0.21, 0.58 ± 0.11, and 0.63 ± 0.26 μM.

Apoptosis Analysis

Cell Line: RAW264.7 cells[1]
Concentration: 0 μM, 0.1 μM, 0.25 μM, 0.5 μM and 1 μM
Incubation Time: 48 h
Result: Induced apoptosis in a dose-dependent manner, with the apoptotic rates of 6.48% (0.1 μM), 7.73% (0.25 μM), 8.60% (0.5 μM) and 9.17% (1 μM).

Cell Cycle Analysis

Cell Line: RAW264.7 cells[1]
Concentration: 0 μM, 0.1 μM, 0.25 μM, 0.5 μM and 1 μM
Incubation Time: 24 h
Result: Led to significant G2 phase arrest in RAW264.7 cells in a dose-dependent manner, the percentage of cells in the G2 phase slightly increased from 10.90% to 90.16% (0-1 μM).

体内研究
(In Vivo)

ATX inhibitor 13 (compound 10c) (C57BL/6J mice, 0-1000 mg/kg, Orally, once) has an acceptable safety profile[1].

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

Animal Model: C57BL/6J mice (5 groups,4 mice per group)[1]
Dosage: 5000, 3200, 2500 and 1000 mg/kg
Administration: Orally, once
Result: Had an acceptable safety profile, showed no obvious safety concerns.

分子量

596.55

Formula

C31H35Cl2N5O3
CAS 号

2485779-34-6
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]. Lei H, et al. Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors. Eur J Med Chem. 2022;236:114307.

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