BLU2864|cas:2810747-89-6|西域试剂

BLU2864,99.24%

产品编号：Bellancom-150076| CAS NO：2810747-89-6| 分子式：C₂₄H₁₉F₃N₄O₂| 分子量：452.43

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-150076		￥8500.00	杭州北京（现货）
Bellancom-150076		￥14500.00	杭州北京（现货）

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BLU2864

产品介绍

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=0.3 nM)。BLU2864 具有抗肿瘤活性，可用于癌症和多囊肾的研究。

生物活性

BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC₅₀=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research.

体外研究

BLU2864 (40 nM and 200 nM; 5 d) inhibits forskolin (HY-15371)-induced in vitro cystogenesis.

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

Cell Viability Assay

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.

体内研究
(In Vivo)

BLU2864 (oral gavage; 45 mg/kg; once daily; 5 d) inhibits renal PKA activity in Pkd1^RC/RC mice.
BLU2864 (oral gavage; 30 mg/kg; once daily; 5 d) inhibits PKA activity and ameliorates PKD in Pkd1^RC/RC mice.
BLU2864 (oral gavage; 30 mg/kg and 75 mg/kg; once daily; 34 d) reduces FLC tumor growth in vivo.

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

Animal Model:	Pkd1^RC/RC mice
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
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
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.

体内研究

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

Animal Model:	Pkd1^RC/RC mice
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
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
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.

体内研究

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

Animal Model:	Pkd1^RC/RC mice
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
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
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.