Avapritinib

别名: BLU-285 中文名称:阿伐普利尼

Avapritinib是一种小分子激酶抑制剂,可有效抑制PDGFRα D842V突变体的活性、在细胞背景下抑制PDGFRα D842V自我磷酸化(IC50=30 nM);同时也是Kit (c-Kit)突变(Kit (c-Kit) D816V)的抑制剂(IC50=0.5 nM)。

Avapritinib Chemical Structure

Avapritinib Chemical Structure

CAS: 1703793-34-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) 3841.53 现货
2mg 1204.09 现货
5mg 2105.79 现货
25mg 6470.97 现货
1g 131614.26 现货
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Avapritinib相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.008 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.01 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.017 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.019 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.022 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.028 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.029 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.034 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.034 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.042 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.069 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.078 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.117 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.167 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.292 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.427 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.751 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.86 μM. 30204441
BA/F3 cells Cytotoxicity assay 72 h Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay, GI50 = 4.075 μM. 30204441
BA/F3 cells Growth inhibiton assay 72 h Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 4.952 μM. 30204441
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生物活性

产品描述 Avapritinib是一种小分子激酶抑制剂,可有效抑制PDGFRα D842V突变体的活性、在细胞背景下抑制PDGFRα D842V自我磷酸化(IC50=30 nM);同时也是Kit (c-Kit)突变(Kit (c-Kit) D816V)的抑制剂(IC50=0.5 nM)。
靶点
PDGFRα (D842V) [1] c-Kit (D816V) [1]
0.5 nM 0.5 nM
体外研究(In Vitro)
体外研究活性

BLU-285是一种选择性的口服抑制剂,靶向KIT Exon 17和PDGFRα D842活化环突变体。BLU-285可在HMC1.2细胞中抑制KIT(D816V),IC50=3 nM;在P815细胞中抑制KIT(D816Y),IC50=22 nM。它还可在Kasumi细胞中抑制KIT Exon 17突变体(如N822K),IC50=40 nM[1]

实验图片 检测方法 检测指标 实验图片 PMID
Western blot PDGFRA / c-KIT / Wee1 / Cdc2 / PARP / γH2AX / CyclinD1 / β-actin 33320833
体内研究(In Vivo)
体内研究活性

在体内,BLU-285是良好的、具有口服生物活性的抑制剂,能在D816Y驱使的移植瘤模型中剂量依赖性地抑制肿瘤的生长。每日给药30 mg/kg,可引起>90%的靶点被抑制,从而引起肿瘤消退。BLU-285可靶向疾病中一些未知的基因组驱动子,为PDGFRα D842V驱动的胃肠道间质瘤或系统性肥大细胞增生症的治疗提供了可能。除了单药活性,BLU-285还可与胃肠道间质瘤治疗中其他试剂组合给药,覆盖全部KIT初级和抗性突变体[1]

动物实验 Animal Models mice
Dosages 10 或 30 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04908176 Completed
Gastrointestinal Stromal Tumors|GIST|Non-resectable Advanced Solid Tumors|Recurrent or Unresectable Central Nervous System (CNS) Tumors
Blueprint Medicines Corporation
August 24 2022 Phase 1
NCT04695431 Completed
Advanced Systemic Mastocytosis|Aggressive Systemic Mastocytosis|Systemic Mastocytosis With an Associated Hematological Neoplasm|Mast Cell Leukemia
Blueprint Medicines Corporation|Analysis Group Inc.
December 2 2020 --
NCT03731260 Active not recruiting
Indolent Systemic Mastocytosis
Blueprint Medicines Corporation
April 16 2019 Phase 2
NCT03580655 Active not recruiting
Advanced Systemic Mastocytosis|Aggressive Systemic Mastocytosis|Systemic Mastocytosis With an Associated Hematologic Neoplasm|Mast Cell Leukemia
Blueprint Medicines Corporation
November 21 2018 Phase 2
NCT03465722 Completed
GIST
Blueprint Medicines Corporation
March 26 2018 Phase 3

化学信息&溶解度

分子量 498.56 分子式

C26H27FN10

CAS号 1703793-34-3 SDF Download Avapritinib SDF
Smiles CC(C1=CC=C(C=C1)F)(C2=CN=C(N=C2)N3CCN(CC3)C4=NC=NN5C4=CC(=C5)C6=CN(N=C6)C)N
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( (200.57 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 1.5 mg/mL (3.0 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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