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首页 / 抑制剂/激动剂 / 蛋白质酪氨酸激酶 / c-Kit / Avapritinib

Avapritinib {[allProObj[0].p_purity_real_show]}

货号：A172367 同义名： BLU-285

BLU-285 is a potent KIT receptor and PDGFRα dual inhibitor with IC50 of 0.27 and 0.24 nM for KIT (D816V) and PDGFRα (D842V) respectively, developed as a highly targeted therapy for SM.

Avapritinib 化学结构 CAS号：1703793-34-3
Avapritinib 化学结构
CAS号：1703793-34-3
Avapritinib 3D分子结构
CAS号：1703793-34-3
Avapritinib 化学结构 CAS号：1703793-34-3
Avapritinib 3D分子结构 CAS号：1703793-34-3
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Avapritinib 纯度/质量文件 产品仅供科研

货号：A172367 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 c-Kit ↓ 其他靶点 纯度
Tyrphostin AG1296 +

c-Kit (Swiss 3T3), IC50: 1.8 μM

 		PDGFR 99%+
Masitinib +

Kit, IC50: 200 nM

 		99%+
Motesanib Diphosphate +++

Kit, IC50: 8 nM

 		98%
Ki8751 ++

c-Kit, IC50: 40 nM

 		98+%
Tivozanib ++

c-Kit, IC50: 78 nM

 		99%+
Pazopanib +

c-Kit, IC50: 140 nM

 		99%
Sitravatinib +++

Kit, IC50: 6 nM

 		99%+
Pexidartinib +++

Kit, IC50: 10 nM

 		99%+
Lactate ++++

c-Kit, IC50: 2 nM

 		FLT3 85%
Amuvatinib +++

c-Kit (D816H), IC50: 10 nM

 		99%+
Imatinib Mesylate +

c-Kit, IC50: 100 nM

 		PDGFR 99%
AZD2932 +++

c-Kit, IC50: 9 nM

 		98%
Axitinib ++++

Kit, IC50: 1.7 nM

 		98%
Dovitinib ++++

c-Kit, IC50: 2 nM

 		FLT3 99%+
Sunitinib ✔ FLT3 98%
OSI-930 +

Kit, IC50: 80 nM

 		99%+
Telatinib ++++

c-Kit, IC50: 1 nM

 		99%+
Dasatinib monohydrate ++

c-Kit (wt), IC50: 79 nM

c-Kit (D816V), IC50: 37 nM

 		Src 98%
Dasatinib ++

c-Kit (wt), IC50: 79 nM

c-Kit (D816V), IC50: 37 nM

 		Src 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Avapritinib 生物活性

靶点

  • PDGFRα

    PDGFRα (D842V), IC50:0.5 nM
描述 Gastrointestinal stromal tumors (GIST) are the largest group of mesenchymal tumors in the intestinal tract. Over 80% of GIST harbors mutations in the c-KIT cell surface transmembrane receptor tyrosine kinase. Mutations in the platelet-derived growth factor receptor α (PDGFRα) gene accounts for 5 - 10% GIST[1]. BLU-285 is a small molecule kinase inhibitor that shows potent inhibitory activity against PDGFRα D842V mutant in vitro with an IC50 value of 0.5 nM. It inhibits the autophosphorylation of PDGFRα D842V in the cellular setting with an IC50 value of 30 nM. BLU-285 also potently inhibits the analogous KIT mutation, D816V in KIT Exon 17, with an IC50 value of 0.5 nM. In cellular assays, BLU-285 potently inhibits KIT D816 mutants D816V (HMC1.2 cells), D816Y (P815 cells), and KIT Exon 17 mutant N822K (Kasumi cells) with IC50 values of 3 nM, 22 nM, and 40 nM, respectively. In a D816Y-driven xenograft model, BLU-285 (30 mg/kg, once daily) resulted in >90% tumor suppression[2].

Avapritinib 动物研究

Dose Mice: 0.3 mg/kg - 30 mg/kg[1] (p.o.)
Administration p.o.

Avapritinib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03465722 GIST Phase 3 Recruiting April 2023 -
NCT03731260 Indolent Systemic Mastocytosis... 展开 >> Smoldering Systemic Mastocytosis 收起 << Phase 2 Not yet recruiting November 2023 -
NCT02508532 Gastrointestinal Stromal Tumor... 展开 >>s (GIST) Other Relapsed or Refractory Solid Tumors 收起 << Phase 1 Recruiting May 2019 United States, California ... 展开 >> Sarcoma Oncology Center Recruiting Santa Monica, California, United States, 90403 United States, Florida Sylvester Comprehensive Cancer Center Recruiting Miami, Florida, United States, 33136 United States, Massachusetts Dana Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 United States, New York Memorial Sloan Kettering Cancer Center Recruiting New York, New York, United States, 10065 United States, Oregon Oregon Health and Science University Recruiting Portland, Oregon, United States, 97239 United States, Pennsylvania Fox Chase Cancer Center Recruiting Philadelphia, Pennsylvania, United States, 19111 United States, Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Belgium Leuven Cancer Institute University Hospitals Leuven Recruiting Leuven, Belgium, 3000 France Centre Leon Berard Recruiting Lyon, France, 69008 Institut Gustave Roussy Recruiting Paris, France, 94805 Germany University of Duisburg-Essen Recruiting Essen, Germany, 45122 Italy Fondazione IRCCS - Istituto Nazinale dei Tumori Recruiting Milan, Italy, 20133 Korea, Republic of Asan Medical Center Recruiting Seoul, Korea, Republic of, 05505 Netherlands Erasmus MC Cancer Institute Recruiting Rotterdam, Netherlands, 3015 Poland Centrum Onkologii-Instytut im. Marii Skłodowskiej-Curie w Warszawie Recruiting Warsaw, Poland, 02-781 Spain Vall d' Hebron Institute of Oncology (VHIO) Recruiting Barcelona, Spain, 08305 United Kingdom Royal Marsden Hospital Recruiting London, United Kingdom, SW3 6JJ 收起 <<

Avapritinib 参考文献

[1]Schneider-Stock R. BLU-285-the breakthrough in treatment of patients with aggressive systemic mastocytosis and gastrointestinal stromal tumor. Ann Transl Med. 2018 Jun;6(11):232. doi: 10.21037/atm.2018.05.21. PMID: 30023395; PMCID: PMC6036000.

[2]BLU-285, the first selective inhibitor of PDGFRα D842V and KIT Exon 17 mutants

Avapritinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.01mL

0.40mL

0.20mL

10.03mL

2.01mL

1.00mL

20.06mL

4.01mL

2.01mL

Avapritinib 技术信息

CAS号1703793-34-3
分子式C26H27FN10
分子量 498.558
别名 BLU-285
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C
溶解度

DMSO: 85 mg/mL(170.49 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

2% DMSO+40% PEG 300+2% Tween 80+water 4 mg/mL

Tags: Avapritinib | 1703793-34-3 | BLU-285 | BLU285 | BLU 285 | KIT/PDGFRA Inhibitor | Protein Tyrosine Kinase/RTK | c-Kit | PDGFR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Avapritinib 纯度/质量文件 | Avapritinib 亚型比较 | Avapritinib 生物活性 | Avapritinib 动物研究 | Avapritinib 临床数据 | Avapritinib 参考文献 | Avapritinib 实验方案 | Avapritinib 技术信息

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