Duvelisib (IPI-145)
别名: INK1197 中文名称：杜韦利西布
Duvelisib (IPI-145, INK1197) 是一种新型选择性PI3K δ/γ抑制剂，在无细胞试验中Ki和IC50分别为 23 pM/243 pM 和 1 nM/50 nM，对 PI3K δ/γ 的选择性比对其它蛋白激酶高。Phase 3。
Duvelisib (IPI-145) Chemical Structure
CAS: 1201438-56-3
产品质控
批次：
纯度：
99.96%
99.96
Duvelisib (IPI-145)相关产品
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 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Duvelisib (IPI-145, INK1197) 是一种新型选择性PI3K δ/γ抑制剂，在无细胞试验中Ki和IC50分别为 23 pM/243 pM 和 1 nM/50 nM，对 PI3K δ/γ 的选择性比对其它蛋白激酶高。Phase 3。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | IPI-145抑制鼠/人类 B细胞增殖，EC50 为0.5 nM/0.5 nM，也抑制人类T细胞增殖，EC50为9.5 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 | PI3Kγ / PI3Kδ p-AKT / AKT / p-MAPK / MAPK |
|
29522278 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | IPI-145 按10 mg/kg剂量口服处理给药小鼠和大鼠，具有良好的药代动力学, Cmax 和AUC分别为390 ng/mL 和 137 ng•h/mL。IPI-145 (10 mg/kg) 有效作用于鼠DTH 模型，约~50% 耳肿胀。IPI-145 (10 mg/kg) 有效作用于大鼠胶原诱导的关节炎（CIA）模型，这种作用具有剂量依赖性。IPI-145 作用于大鼠CIA模型，防止发炎，且保护关节骨和软骨。IPI-145 (10 mg/kg,QD)有效作用于大鼠佐剂性多关节炎模型。[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 |
化学信息&溶解度
| 分子量 | 416.86 | 分子式 | C22H17ClN6O |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 83 mg/mL ( (199.1 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : 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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常见问题及建议解决方法
问题 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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