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Avapritinib
別名: BLU-285 中文名稱：阿伐普利尼
Avapritinib是一種小分子激酶抑制劑，可有效抑制PDGFRα D842V突變體的活性、在細胞背景下抑制PDGFRα D842V自我磷酸化（IC50=30 nM）；同時也是Kit (c-Kit)突變（Kit (c-Kit) D816V）的抑制劑（IC50=0.5 nM）。
Avapritinib Chemical Structure
CAS: 1703793-34-3
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
Avapritinib相關(guān)產(chǎn)品
| 相關(guān)靶點 | PDGFRα PDGFRβ | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Crenolanib CP-673451 Orantinib (SU6668) Tyrphostin AG 1296 Trapidil PP121 AZD2932 | 點擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫 細胞周期化合物庫 血管生成相關(guān)化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | |
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Avapritinib是一種小分子激酶抑制劑，可有效抑制PDGFRα D842V突變體的活性、在細胞背景下抑制PDGFRα D842V自我磷酸化（IC50=30 nM）；同時也是Kit (c-Kit)突變（Kit (c-Kit) D816V）的抑制劑（IC50=0.5 nM）。 | ||||
|---|---|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | BLU-285是一種選擇性的口服抑制劑，靶向KIT Exon 17和PDGFRα D842活化環(huán)突變體。BLU-285可在HMC1.2細胞中抑制KIT(D816V)，IC50=3 nM；在P815細胞中抑制KIT(D816Y)，IC50=22 nM。它還可在Kasumi細胞中抑制KIT Exon 17突變體（如N822K），IC50=40 nM[1]。 |
|||
|---|---|---|---|---|
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | PDGFRA / c-KIT / Wee1 / Cdc2 / PARP / γH2AX / CyclinD1 / β-actin |
|
33320833 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 在體內(nèi)，BLU-285是良好的、具有口服生物活性的抑制劑，能在D816Y驅(qū)使的移植瘤模型中劑量依賴性地抑制腫瘤的生長。每日給藥30 mg/kg，可引起>90%的靶點被抑制，從而引起腫瘤消退。BLU-285可靶向疾病中一些未知的基因組驅(qū)動子，為PDGFRα D842V驅(qū)動的胃腸道間質(zhì)瘤或系統(tǒng)性肥大細胞增生癥的治療提供了可能。除了單藥活性，BLU-285還可與胃腸道間質(zhì)瘤治療中其他試劑組合給藥，覆蓋全部KIT初級和抗性突變體[1]。 |
|
|---|---|---|
| 動物實驗 | 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 |
化學信息&溶解度
| 分子量 | 498.56 | 分子式 | C26H27FN10 |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 100 mg/mL ( (200.57 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 1.5 mg/mL (3.0 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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