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Chiauranib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Chiauranib图片
CAS NO:1256349-48-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
CS2164
产品介绍
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 (VEGFR1VEGFR2VEGFR3PDGFRαc-Kit),有丝分裂相关激酶Aurora B和慢性炎症相关激酶CSF-1RIC50值为 1-9 nM。Chiauranib 具有很强的抗癌作用。
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,PDGFRαandc-Kit), mitosis-related kinaseAurora B, and chronic inflammation-related kinaseCSF-1R, withIC50values 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].

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].

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

性状

Solid

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 mg5 mg10 mg
1 mM2.2964 mL11.4818 mL22.9637 mL
5 mM0.4593 mL2.2964 mL4.5927 mL
10 mM0.2296 mL1.1482 mL2.2964 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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-CDin 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 μL20% 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本网站选购。