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BLU2864

产品编号 T60170 CAS 2810747-89-6

BLU2864 是一种具有口服活性的、高选择性的、ATP 竞争性的 PRKACA 抑制剂，IC50值为0.3 nM。BLU2864 具有抗肿瘤活性，具有用于癌症和多囊肾的研究潜力。

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BLU2864, CAS 2810747-89-6

规格	价格/CNY	货期
1 mg	￥ 995	现货
5 mg	￥ 2,490	现货
10 mg	￥ 3,990	现货
25 mg	￥ 6,390	现货
50 mg	￥ 8,750	现货
100 mg	￥ 11,700	现货
500 mg	￥ 23,600	现货

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选择批次

纯度: 99.73% ee: 100%

纯度: 99.42%

纯度: 97.58%

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor with IC 50 of 0.3 nM. BLU2864 exhibits anti-tumor activity. BLU2864 has potential to be used in cancer and polycystic kidney disease research [1] [2].
体外活性	BLU2864 (40 nM and 200 nM; 5 d) shows inhibition of forskolin -induced cystogenesis in vitro[1]. Cell Viability Assay [1] Cell Line: mIMCD3 cells Concentration: 40 nM and 200 nM Incubation Time: 5 days Result: Inhibited forskolin induced in vitro cystogenesis of mIMCD3 cells cultured in Matrigel by 72% and 100% at 40 and 200 nM concentrations, respectively, relative to control.
体内活性	BLU2864 (oral gavage; 45 mg/kg; once daily; 5 d) shows inhibition of renal PKA activity in Pkd1 RC/RC mice [1]. BLU2864 (oral gavage; 30 mg/kg; once daily; 5 d) inhibits PKA activity and ameliorates PKD in Pkd1 RC/RC mice [1]. BLU2864 (oral gavage; 30 mg/kg and 75 mg/kg; once daily; 34 d) reduces FLC tumor growth in vivo [2]. Animal Model: Pkd1 RC/RC mice [1] Dosage: 45 mg/kg Administration: Oral gavage; 45 mg/kg; once daily; 5 days Result: Suppressed kidney basal and total PKA activities by 74% and 87% at 3 hours and by 46% and 56% at 15 hours, respectively, in the BLU2864-treated mice compared with controls. Animal Model: Pkd1 RC/RC mice [1] Dosage: 30 mg/kg Administration: Oral gavage; 30 mg/kg; once daily; 5 days Result: Showed higher urine outputs at 15 weeks in the BLU2864-treated mice than in the controls. Showed lower kidney weights, kidney volumes as percent of body weights, and cyst indices. Showed renal basal and total PKA activities by 69% and 84% lower in the BLU2864-treated mice compared with controls. Animal Model: Mice harboring FLC PDX tumors [2] Dosage: 30 mg/kg and 75 mg/kg Administration: Oral gavage; 30 mg/kg and 75 mg/kg; once daily; 34 days Result: Inhibited tumor growth by 48.5% (P=0.003) and by 45.3% (P=0.0005), respectively, at day 34.

分子量	452.43
分子式	C24H19F3N4O2
CAS No.	2810747-89-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (110.51 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2103 mL	11.0514 mL	22.1029 mL	55.2572 mL
	5 mM	0.4421 mL	2.2103 mL	4.4206 mL	11.0514 mL
	10 mM	0.221 mL	1.1051 mL	2.2103 mL	5.5257 mL
	20 mM	0.1105 mL	0.5526 mL	1.1051 mL	2.7629 mL
	50 mM	0.0442 mL	0.221 mL	0.4421 mL	1.1051 mL
	100 mM	0.0221 mL	0.1105 mL	0.221 mL	0.5526 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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参考文献

1. Xiaofang Wang, et al. Protein Kinase A Downregulation Delays the Development and Progression of Polycystic Kidney Disease. J Am Soc Nephrol. 2022 Jun;33(6):1087-1104. 2. Stefanie S. Schalm, et al. Evaluation of PRKACA as a Therapeutic Target for Fibrolamellar Carcinoma. bioRxiv 2022.01.31.477690.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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