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Ripretinib
別名: DCC-2618
Ripretinib是一種具有口服活性的Kit (c-Kit)和PDGFR-alpha抑制劑，對WT Kit (c-Kit)、V654A Kit (c-Kit)、T670I Kit (c-Kit)、D816H Kit (c-Kit)和D816V Kit (c-Kit)的IC50分別為4 nM、8 nM、18 nM、5 nM和14 nM。
Ripretinib Chemical Structure
CAS: 1442472-39-0
產(chǎn)品質(zhì)控
批次：
純度：
99.82%
99.82
Ripretinib相關(guān)產(chǎn)品
| 相關(guān)產(chǎn)品 | Masitinib Amuvatinib (MP-470) OSI-930 Sitravatinib (MGCD516) ISCK03 PDGFR inhibitor 1 | 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 |
|---|---|---|---|---|---|
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.003 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.004 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.004 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.006 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.013 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | Inhibition of Kit exon 11 deletion (557 to 558 residues) 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 = 0.014 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.023 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.031 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.034 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.037 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.037 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.04 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.045 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.048 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.075 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.078 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.098 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.13 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.188 μM. | 30204441 | |
| Growth inhibition assay | BA/F3 | 72 hrs | 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 = 0.205 μM. | 30204441 | |
| Cytotoxicity assay | BA/F3 | 72 hrs | Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay, GI50 = 8.037 μM. | 30204441 | |
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Ripretinib是一種具有口服活性的Kit (c-Kit)和PDGFR-alpha抑制劑，對WT Kit (c-Kit)、V654A Kit (c-Kit)、T670I Kit (c-Kit)、D816H Kit (c-Kit)和D816V Kit (c-Kit)的IC50分別為4 nM、8 nM、18 nM、5 nM和14 nM。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | DCC-2618有效并廣泛地抑制KIT原發(fā)性和耐藥性突變體，如發(fā)生在外顯子9、11、13、14、17和18的突變，以及發(fā)生在PDGFRA外顯子12、14、18的原發(fā)性突變[3]。DCC-2618以納摩爾級別的效力抑制多種性質(zhì)的KIT：WT (IC50 4 nM), V654A (8 nM), T670I (18 nM), D816H (5 nM), D816V (14 nM)。在瞬時轉(zhuǎn)染了KIT原發(fā)性突變體和二次突變的CHO細胞中，DCC-2618抑制了外顯子17、外顯子9/13、外顯子9/14，外顯子9/17，外顯子11/17突變的KIT，包括位于外顯子17的D816V, D816G, D820A, D820E, D820Y, N822K, N822Y, N822H和Y823D原發(fā)性或二次突變。在MO7e細胞系中，DCC-2618抑制野生型KIT的磷酸化（IC50=36 nM）。在人源GIST細胞系中，包括GIST T1(缺失外顯子11)、GIST 430（缺失外顯子11/外顯子13 V654A）和GIST 48（外顯子11 V560D/外顯子17 D820A）, DCC-2618也能有效抑制KIT的激活。在小鼠肥大細胞增多癥中，DCC-2618可有效抑制P815細胞(表達外顯子17 D816Y 突變KIT)的增殖，IC50為2 nM[1]。在多種人類肥大細胞系（HMC-1, ROSA, MCPV-1）和從晚期系統(tǒng)性肥大細胞增多癥患者體內(nèi)分離的原代腫瘤肥大細胞中，DCC-2618可抑制其增殖和生存[2]。 |
|||
|---|---|---|---|---|
| 細胞實驗 | 細胞系 | HMC-1.1, HMC-1.2, ROSA (KIT WT)和 ROSA (KIT D816V)細胞 | ||
| 濃度 | 0.5-5 μM | |||
| 孵育時間 | 4 h | |||
| 方法 | 將細胞培養(yǎng)于對照組培養(yǎng)基中或加入0.5-5 μM DCC-2618，置于37℃培養(yǎng)4小時。結(jié)束后，收集細胞提取蛋白質(zhì)，進行Western blotting分析。 |
|||
| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
| Western blot | KIT / BTK STAT5 / AKT / ERK |
|
29439183 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 在體內(nèi)，50 mg/kg DCC-2618可在GIST T1移植瘤模型抑制KIT磷酸化，達到90%的有效劑量（ED90），EC50約為470 ng/mL。每日兩次口服給藥，DCC-2618可幾乎完全地造成腫瘤瘀滯[1]。在移植瘤模型中，DCC-2618可阻止KIT和PFGFRA驅(qū)動的腫瘤生長[3]。 |
|
|---|---|---|
| 動物實驗 | Animal Models | 小鼠移植瘤模型 |
| Dosages | 100 mg/kg/day 或 25 mg/kg/day 或 50 mg/kg BID | |
| Administration | 口服 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05080621 | Withdrawn | Gastrointestinal Stromal Tumors |
Deciphera Pharmaceuticals LLC |
November 2021 | Phase 1|Phase 2 |
| NCT04633122 | Completed | Gastrointestinal Stromal Tumor(GIST) |
Zai Lab (Shanghai) Co. Ltd.|Zai Lab (Hong Kong) Ltd. |
November 25 2020 | Phase 2 |
| NCT02571036 | Completed | Gastrointestinal Stromal Tumors|Advanced Systemic Mastocytosis|Advanced Cancers |
Deciphera Pharmaceuticals LLC |
November 2015 | Phase 1 |
化學(xué)信息&溶解度
| 分子量 | 510.36 | 分子式 | C24H21BrFN5O2 |
| CAS號 | 1442472-39-0 | SDF | -- |
| Smiles | CCN1C2=CC(=NC=C2C=C(C1=O)C3=CC(=C(C=C3Br)F)NC(=O)NC4=CC=CC=C4)NC | ||
| 儲存條件(自收到貨起) | 3年 -20°C 粉狀 | ||
|
體外溶解度 |
DMSO : 100 mg/mL ( (195.94 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : 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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