Cenisertib(Synonyms: AS-703569; R-763)

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Cenisertib (Synonyms: AS-703569; R-763) 纯度: 99.56%

Cenisertib (AS-703569) 是一种 ATP 竞争性的多激酶抑制剂，可抑制 Aurora-kinase-A/B，ABL1，AKT，STAT5, FLT3 的活性。Cenisertib 通过抑制肿瘤肥大细胞 (MC) 中几种不同分子靶标的活性抑制其生长。Cenisertib 抑制异种移植模型中胰腺癌，乳腺癌，结肠癌，卵巢癌和肺癌以及白血病的肿瘤生长。

Cenisertib(Synonyms: AS-703569; R-763)

Cenisertib Chemical Structure

CAS No. : 871357-89-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3850 In-stock
5 mg ￥3500 In-stock
10 mg ￥5500 In-stock
50 mg ￥16500 In-stock
100 mg ￥22500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia[1][2][3].

IC50 & Target[1]

Aurora-A

 

Aurora-B

 

ABL1

 

Akt

 

STAT5

 

体外研究
(In Vitro)

Cenisertib (AS-703569) (1-1000 nM; for 48 hours) induces dose-dependent inhibition of proliferation in primary neoplastic mast cells (MC) [1].
Cenisertib (5-100 nM; for 24 hours) induces a substantial G2/M cell cycle arrest at low nanomolar concentrations in all MC lines[1].
Cenisertib (1-1000 nM; for 24 hours)induces apoptosis in HMC-1.1, HMC-1.2, C2, and NI-1 cells in a dose-dependent manner[1].
Cenisertib (5-500 nM; for 24 hours) induces cleavage of caspase 3 in both HMC-1 sub-clones as well as in C2 and NI-1 cells[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 Proliferation Assay[1]

Cell Line: HMC-1.1, HMC-1.2, ROSAKIT WT, ROSAKIT D816V and MCPV-1.1 mast cells
Concentration: 1, 5, 10, 50, 100, 500, 1000 nM
Incubation Time: 48 hours
Result: Induced dose-dependent inhibition of proliferation in primary neoplastic MC.

Cell Cycle Analysis[1]

Cell Line: HMC-1.1, HMC-1.2, C2 and NI-1 cells
Concentration: 5, 10, 50, 100 nM
Incubation Time: 24 hours
Result: Induced a substantial G2/M cell cycle arrest at low nanomolar concentrations in all MC lines.

Apoptosis Analysis[1]

Cell Line: HMC-1.1, HMC-1.2, C2 and NI-1 cells
Concentration: 1, 5, 10, 50, 100, 500, 1000 nM
Incubation Time: 24 hours
Result: Induced apoptosis in HMC-1.1, HMC-1.2, C2, and NI-1 cells in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: HMC-1.1, HMC-1.2, C2 and NI-1 cells
Concentration: 50, 100, 500 nM
Incubation Time: 24 hours
Result: Induced cleavage of caspase 3 in both HMC-1 sub-clones as well as in C2 and NI-1 cells.

体内研究
(In Vivo)

Cenisertib (AS-703569) (orally; 7 or 10 mg/kg/day; for 3 days followed by a 4-day rest period; for 4 weeks) significantly suppresses tumor growth.

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 CB17 Severe Combined Immunodeficiency (SCID) mice bearing NCI-MDR tumors[2]
Dosage: 7 and 10 mg/kg
Administration: Orally; daily; for 3 days followed by a 4-day rest period; for 4 weeks
Result: Suppressed significantly tumor growth.

Clinical Trial

分子量

451.54

Formula

C24H30FN7O
CAS 号

871357-89-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (553.66 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2146 mL 11.0732 mL 22.1464 mL
5 mM 0.4429 mL 2.2146 mL 4.4293 mL
10 mM 0.2215 mL 1.1073 mL 2.2146 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。-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    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.61 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 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.61 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
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.61 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    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玉米油中，混合均匀。

*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]. Peter B, et al. Drug-induced inhibition of phosphorylation of STAT5 overrides drug resistance in neoplastic mast cells. Leukemia. 2018 Apr;32(4):1016-1022.

    [2]. McLaughlin J, et al. Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen. J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113.

    [3]. Maryam Shariati, et al. Targeting AKT for cancer therapy. Expert Opin Investig Drugs. 2019 Nov;28(11):977-988.

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