1. Cell Cycle/DNA Damage Cytoskeleton
  2. Kinesin
  3. ATX020

ATX020 是一种强效、选择性且具有口服活性的驱动蛋白 KIF18A 抑制剂。ATX020 可抑制人类、大鼠和犬类中 KIF18A 的 ATP 酶活性,其 IC50 值分别为 0.11 μM、0.16 μM 和 0.24 μM。ATX020 对其他运动蛋白 (CENP-E、Eg5、KIF15 等) 具有高选择性,其 IC50 值大于 10 μM,仅对 KIF19 具有较弱的抑制作用 (IC50 值为 6.1 μM)。ATX020 能够抑制癌细胞增殖。

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ATX020

ATX020 Chemical Structure

CAS No. : 3030452-08-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ATX020 is a potent, selective and orally active kinesin KIF18A inhibitor. ATX020 inhibits the ATPase activity of KIF18A in humans, rats and dogs, with IC50 values of 0.11 μM, 0.16 μM and 0.24 μM, respectively. ATX020 shows high selectivity for other motor proteins (CENP-E, Eg5, KIF15, etc.), with IC50 values >10 μM and only has a weak inhibitory effect on KIF19 (IC50 = 6.1 μM). ATX020 can inhibit cancer cells proliferation[1].

体外研究
(In Vitro)

ATX020 (7 days) 对染色体不稳定性阳性 (CIN+) 癌细胞 (OVCAR-3, OVCAR-8, AU565) 有强效抑制作用,IC50 分别为 0.090 μM、0.53 μM、0.21 μM;对 CIN- 癌细胞 (OVK18, A2780, CAL51) 抑制活性低,IC50 ≥8.8 μM[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

ATX020 (30-100 mg/kg,口服,每日一次,连续 28 天) 可抑制携带 OVCAR-3/OVK18 肿瘤异种移植的雌性 Balb/C 裸鼠的肿瘤生长[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Balb/C nude mice bearing OVCAR-3 CDX tumors[1]
Dosage: 30 and 100 mg/kg
Administration: Orally administration, once daily for 28 days
Result: Ahieves 94% and 104% tumor growth inhibition of OVCAR-3.
分子量

581.75

Formula

C26H37F2N5O4SSi

CAS 号
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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ATX020
目录号:
HY-179210
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