aladdin 阿拉丁 A407922 阿伐普利替尼（BLU-285） 1703793-34-3 10mM in DMSO

中文名：阿伐普利替尼（BLU-285）

英文名：Avapritinib (BLU-285)

纯度：Moligand™，≥98%

货号：A414052

Cas号：1703793-34-3

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibitsPDGFRα D842Vmutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogousKit (c-Kit)mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM).

Targets

PDGFRα (D842V) ; c-Kit (D816V) 0.5 nM; 0.5 nM

In vitro

BLU-285 is a selective oral inhibitor that targets KIT Exon 17 and PDGFRα D842 activation loop mutants. Cellular assays measuring inhibition of KIT mutant autophosphorylation confirm the activity of BLU-285 against the KIT D816 mutants D816V (HMC1.2 cells, IC50 = 3 nM) and D816Y (P815 cells, IC50 = 22 nM) as well as other KIT Exon 17 mutants such as N822K (Kasumi cells, IC50 = 40 nM) found in treatment-refractory GIST.

In vivo

BLU-285 is a well-tolerated, orally bioavailable agent that achieves dose dependent tumor growth inhibition in a D816Y-driven xenograft model. A PK-PD-efficacy relationship with BLU-285 has been established demonstrating that tumor regression results from >90% target suppression and is observed with 30 mg/kg once daily dosing. With potent activity against PDGFRα D842V and KIT Exon 17 mutants, BLU-285 targets previously unaddressed genomic drivers of disease and provides promise for the treatment of PDGFRα D842V-driven GIST(gastrointestinal stromal tumor) or SM(systemic mastocytosis), where more than 90% of patients carry the KIT D816V mutation. Besides single agent activity, the highly selective BLU-285 offers an opportunity for combination with other agents in GIST to cover the entirety of KIT primary and resistance mutants.

查看阿拉丁官网此产品相关对应页面：https://www.aladdin-e.com/zh_cn/A414052.html