Chiauranib(Synonyms: CS2164)

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Chiauranib (Synonyms: CS2164) 纯度: 99.28%

Chiauranib (CS2164) 是一种针对肿瘤血管生成的具有口服活性的多靶点抑制剂。Chiauranib 有效抑制血管生成相关激酶 (VEGFR1，VEGFR2，VEGFR3，PDGFRα 和 c-Kit)，有丝分裂相关激酶 Aurora B 和慢性炎症相关激酶 CSF-1R，IC50 值为 1-9 nM。Chiauranib 具有很强的抗癌作用。

Chiauranib(Synonyms: CS2164)

Chiauranib Chemical Structure

CAS No. : 1256349-48-0

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2750 In-stock
5 mg ￥2500 In-stock
10 mg ￥4500 In-stock
25 mg ￥8500 In-stock
50 mg ￥13500 In-stock
100 mg ￥19500 In-stock
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生物活性

Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects[1].

IC50 & Target[1]

Flt-1

8 nM (IC50)

KDR

7 nM (IC50)

Flt-4

9 nM (IC50)

PDGFRα

1 nM (IC50)

Aurora B

9 nM (IC50)

PDGFRβ

93 nM (IC50)

c-Kit

4 nM (IC50)

CSF-1R

7 nM (IC50)

体外研究
(In Vitro)

Chiauranib (CS2164; 3 μM; 24 hours) shows induction of G2/M cell cycle arrest and suppression of cell proliferation in tumor tissues through the inhibition of Aurora B-mediated H3 phosphorylation[1].
In HUVEC and PDGFRβ phosphorylation in PDGFRβ overexpressed NIH3T3 cells, Chiauranib (CS2164; 0.03-3 μM) displays anti-angiogenic activities through suppression of VEGFR/PDGFR phosphorylation, inhibition of ligand-dependent cell proliferation and capillary tube formation, and prevention of vasculature formation in tumor tissues[1].
. Chiauranib (CS2164) inhibits CSF-1R phosphorylation that leads to the suppression of ligand-stimulated monocyte-to-macrophage differentiation and reduces CSF-1R+ cells in tumor tissues[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: Molt-4 cells
Concentration: 3 μM
Incubation Time: 24 hours
Result: Induced the pronounced cell cycle arrest in the G2/M phase at 3 μM.

Western Blot Analysis[1]

Cell Line: Molt-4 cells
Concentration: 1.5 μM, 3 μM, 6 μM
Incubation Time: 24 hours
Result: Yielded a substantial reduction in the level of p-H3 in Molt‐4 cells in a concentration-dependent fashion.

体内研究
(In Vivo)

Chiauranib (CS2164; 0.5-40 mg/kg; oral administration; once daily; for 33 days or 43 days) treatment induces remarkable regression or complete inhibition of tumor growth at well-tolerated oral doses in several human tumor xenograft models. Chiauranib exhibits broad and potent in vivo anti-tumor activities[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c athymic (nu+/nu+) mice (6-week old) bearing HCT-8, SMMC-7721, MGC‐803 or A549 cells[1]
Dosage: 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg
Administration: Oral administration; once daily; for 33 days or 43 days
Result: Induced remarkable regression or complete inhibition of tumor growth in several human tumor xenograft models.

Clinical Trial

分子量

435.47

Formula

C27H21N3O3
CAS 号

1256349-48-0
中文名称

西奥罗尼
运输条件

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (143.52 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2964 mL 11.4818 mL 22.9637 mL
5 mM 0.4593 mL 2.2964 mL 4.5927 mL
10 mM 0.2296 mL 1.1482 mL 2.2964 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.78 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.78 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. You Zhou, et al. CS2164, a novel multi-target inhibitor against tumor angiogenesis, mitosis and chronic inflammation with anti-tumor potency. Cancer Sci. 2017 Mar;108(3):469-477.

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