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
CAS: 1703793-34-3
产品质控
批次：
纯度：
99.99%
99.99
Avapritinib相关产品
| 相关靶点 | PDGFRα PDGFRβ | 点击展开 |
|---|---|---|
| 相关产品 | Crenolanib CP-673451 Orantinib (SU6668) Tyrphostin AG 1296 Trapidil PP121 AZD2932 | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库 细胞周期化合物库 血管生成相关化合物库 | 点击展开 |
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 | |
| 点击查看更多细胞系数据 | |||||
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 |
|
| 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]。 |
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|---|---|---|---|---|
| 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]。 |
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|---|---|---|
| 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) | |||
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体外溶解度 |
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 |
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体内溶解度 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
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
只
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，注：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：取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：取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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