Chiauranib Ibcasertib; CS2164|cas:1256349-48-0|西域试剂

Chiauranib Ibcasertib; CS2164,99.28%

产品编号：Bellancom-124526| CAS NO：1256349-48-0| 分子式：C₂₇H₂₁N₃O₃| 分子量：435.47

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货号	价格	库存与货期
Bellancom-124526	￥2500.00	杭州北京（现货）
Bellancom-124526	￥4500.00	杭州北京（现货）
Bellancom-124526	￥8500.00	杭州北京（现货）
Bellancom-124526	￥13500.00	杭州北京（现货）
Bellancom-124526	￥19500.00	杭州北京（现货）

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Chiauranib Ibcasertib; 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 (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。

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.

体外研究

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.
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.
. 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.

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

Cell Cycle Analysis

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

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.

西域 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
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.

体内研究

西域 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
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.

体内研究

西域 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
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.

性状

Solid

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