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Duvelisib (IPI-145)
別名: INK1197 中文名稱：杜韋利西布
Duvelisib (IPI-145, INK1197) 是一種新型選擇性PI3K δ/γ抑制劑，在無細胞試驗中Ki和IC50分別為 23 pM/243 pM 和 1 nM/50 nM，對 PI3K δ/γ 的選擇性比對其它蛋白激酶高。Phase 3。
Duvelisib (IPI-145) Chemical Structure
CAS: 1201438-56-3
產(chǎn)品質控
批次：
純度：
99.96%
99.96
Duvelisib (IPI-145)相關產(chǎn)品
相關信號通路圖
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 |
|---|---|---|---|---|---|
| BJAB | Cell viability assay | 0.1, 1, 5 μM | 48 and 72 h | inhibited cell growth | 29522278 |
| LCL | Cell viability assay | 0.1, 1, 5 μM | 48 and 72 h | inhibited cell growth | 29522278 |
| Ramos460 | Function assay | 1 μM | effectively impaired the phosphorylation of Akt | 30584254 | |
| Raji32 | Function assay | 1 μM | effectively impaired the phosphorylation of Akt | 30584254 | |
| MOLT3 | Function assay | 0.1, 1.0, and 9.0 μM | IPI145 was able to inhibit Akt and S6 phosphorylation but barely affected the growth of MOLT3 T-ALL | 30970263 | |
| JURKAT | Function assay | 0.1, 1.0, and 9.0 μM | IPI145 was able to inhibit Akt and S6 phosphorylation and modestly affected growth in JURKAT | 30970263 | |
| Loucy | Proliferation assay | 3 days | Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay, IC50=0.98 μM | 27774127 | |
| MOLM14 | Proliferation assay | 3 days | Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay, IC50=1.2 μM | 27774127 | |
| MV4-11 | Proliferation assay | 3 days | Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay, IC50=4.4 μM | 27774127 | |
| MOLT4 | Proliferation assay | 3 days | Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay, IC50=2.3 μM | 27774127 | |
| Jurkat | Proliferation assay | 3 days | Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay, IC50=1.9 Μm | 27774127 | |
| insect cells | Function assay | 5 mins | Inhibition of recombinant human C-terminal His6-tagged p110gamma expressed in insect cells using phosphatidylinositol as substrate in presence of gamma-32P-ATP after 5 mins by thin layer chromatographic method, IC50 = 0.1 μM. | ChEMBL | |
| Sf21 | Function assay | 5 mins | Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length p85alpha expressed in baculovirus infected Sf21 cells using phosphatidylinositol as substrate in presence of gamma-32P-ATP after 5 mins by thin l, IC50 = 0.1 μM. | ChEMBL | |
| splenic B | Antiproliferative assay | 30 mins | Antiproliferative activity against Balb/c mouse splenic B cells preincubated for 30 mins followed by LPS or F(ab')2 donkey anti-mouse IgM and recombinant mouse IL4 stimulation measured after 72 hrs by Alamar Blue reduction assay, EC50 = 0.1 μM. | ChEMBL | |
| Sf21 | Function assay | 5 mins | Inhibition of N-terminal His6-tagged recombinant full-length human p110beta/untagged recombinant full length p85alpha expressed in baculovirus infected Sf21 cells using phosphatidylinositol as substrate in presence of gamma-32P-ATP after 5 mins by thin la, IC50 = 1 μM. | ChEMBL | |
| Sf21 | Function assay | 5 mins | Inhibition of N-terminal His6-tagged recombinant full-length human p110alpha/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 cells using phosphatidylinositol as substrate in presence of gamma-32P-ATP after 5 mins by , IC50 = 10 μM. | ChEMBL | |
| OCI-Ly3 | Growth inhibition assay | GI50=3.7 μM | 30067771 | ||
| HBL-1 | Growth inhibition assay | GI50=5.3 μM | 30067771 | ||
| TMD-8 | Growth inhibition assay | GI50=0.0005 μM | 30067771 | ||
| U-2932 | Growth inhibition assay | GI50=1.8 μM | 30067771 | ||
| Farage | Growth inhibition assay | GI50=0.04 μM | 30067771 | ||
| SU-DHL-10 | Growth inhibition assay | GI50=2.4 μM | 30067771 | ||
| SU-DHL-4 | Growth inhibition assay | GI50=0.2 μM | 30067771 | ||
| Karpas-422 | Growth inhibition assay | GI50=0.1 μM | 30067771 | ||
| DOHH-2 | Growth inhibition assay | GI50=0.05 μM | 30067771 | ||
| WSU-NHL | Growth inhibition assay | GI50=0.008 μM | 30067771 | ||
| Jeko-1 | Growth inhibition assay | GI50=1.3 μM | 30067771 | ||
| Mino | Growth inhibition assay | GI50=3.4 μM | 30067771 | ||
| NCI-H929 | Growth inhibition assay | GI50=1 μM | 30067771 | ||
| HH | Growth inhibition assay | GI50=0.01 μM | 30067771 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Duvelisib (IPI-145, INK1197) 是一種新型選擇性PI3K δ/γ抑制劑，在無細胞試驗中Ki和IC50分別為 23 pM/243 pM 和 1 nM/50 nM，對 PI3K δ/γ 的選擇性比對其它蛋白激酶高。Phase 3。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | IPI-145抑制鼠/人類 B細胞增殖，EC50 為0.5 nM/0.5 nM，也抑制人類T細胞增殖，EC50為9.5 nM。[1] |
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|---|---|---|---|---|
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | PI3Kγ / PI3Kδ p-AKT / AKT / p-MAPK / MAPK |
|
29522278 | |
| 體內研究(In Vivo) | ||
| 體內研究活性 | IPI-145 按10 mg/kg劑量口服處理給藥小鼠和大鼠，具有良好的藥代動力學, Cmax 和AUC分別為390 ng/mL 和 137 ng•h/mL。IPI-145 (10 mg/kg) 有效作用于鼠DTH 模型，約~50% 耳腫脹。IPI-145 (10 mg/kg) 有效作用于大鼠膠原誘導的關節(jié)炎（CIA）模型，這種作用具有劑量依賴性。IPI-145 作用于大鼠CIA模型，防止發(fā)炎，且保護關節(jié)骨和軟骨。IPI-145 (10 mg/kg,QD)有效作用于大鼠佐劑性多關節(jié)炎模型。[1] |
|
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02307461 | Completed | Healthy |
SecuraBio |
November 2014 | Phase 1 |
| NCT02095587 | Completed | Hepatic Impairment |
SecuraBio |
March 2014 | Phase 1 |
| NCT01947777 | Completed | Healthy |
SecuraBio |
October 2013 | Phase 1 |
| NCT01925911 | Completed | Healthy |
SecuraBio |
August 2013 | Phase 1 |
| NCT01836861 | Completed | Healthy |
SecuraBio |
March 2013 | Phase 1 |
| NCT01549106 | Completed | Healthy Volunteers |
SecuraBio |
August 2011 | Phase 1 |
化學信息&溶解度
| 分子量 | 416.86 | 分子式 | C22H17ClN6O |
| CAS號 | 1201438-56-3 | SDF | Download Duvelisib (IPI-145) SDF |
| Smiles | CC(C1=CC2=C(C(=CC=C2)Cl)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 83 mg/mL ( (199.1 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 |
動物體內配方計算器 | ||||
實驗計算
動物體內配方計算器（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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常見問題及建議解決方法
問題 1:
Whether IPI-145 S7028 is mixture of two chiral forms, if not, which form is it?
回答：
S7028 IPI-145 is S form.
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