计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
阿伐普利替尼（BLU-285）, 血小板衍生生长因子受体 alpha 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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
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
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.
Cell Data
cell lines：Wild-type and mLST8 deficient MEFs
Concentrations：
Incubation Time：
Powder Purity:≥98%
规格
英文别名
5-Pyrimidinemethanamine, α-(4-fluorophenyl)-α-methyl-2-[4-[6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]-1-piperazinyl]-, (αS)-
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Avapritinib (BLU-285)
生化机理
阿伐替尼（BLU-285）是一种小分子激酶抑制剂，在体外能有效抑制 PDGFRα D842V 突变体的活性（IC50 = 0.5 nM），在细胞环境中能有效抑制 PDGFRα D842V 自身磷酸化（IC50 = 30 nM）；同时也是类似 Kit（c-Kit）突变的有效抑制剂，即 Kit（c-Kit）外显子 17 中的 D816V（IC50 = 0.5 nM）。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
血小板衍生生长因子受体 alpha 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C[C@](C1=CC=C(C=C1)F)(C2=CN=C(N=C2)N3CCN(CC3)C4=NC=NN5C4=CC(=C5)C6=CN(N=C6)C)N
分子量
498.56
Reaxy-Rn
28010820
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=28010820&ln=
技术文档
高级数据
产品属性
| IC50 | PDGFRα (D842V), IC50: 0.5 nM |
|---|---|
| ALogP | 1.9 |
关联靶点（人）
KIT
Tclin
肥大细胞/干细胞生长因子受体试剂盒(Mast/stem cell growth factor receptor Kit)
(0 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 30 mg/mL (118.92 mM); Water: Insoluble; Ethanol: Insoluble;
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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