- 抑制劑
- 研究領(lǐng)域
- PI3K/Akt/mTOR信號(hào)通路
- 表觀遺傳
- 甲基化
- 免疫&炎癥
- 酪氨酸蛋白激酶
- 血管生成
- 凋亡
- 自噬
- 內(nèi)質(zhì)網(wǎng)應(yīng)激&UPR響應(yīng)
- JAK/STAT信號(hào)通路
- MAPK信號(hào)通路
- 細(xì)胞骨架
- 細(xì)胞周期
- TGF-beta/Smad信號(hào)通路
- DNA損傷/DNA修復(fù)
- 化合物庫(kù)
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細(xì)胞核與細(xì)胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲(chǔ)液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
- 動(dòng)物實(shí)驗(yàn)
- 鼠尾直接PCR試劑盒(快速基因型鑒定)
- 小鼠CD3+ T細(xì)胞分選試劑盒
- 小鼠CD4+ T細(xì)胞分選試劑盒
- 小鼠CD8+ T細(xì)胞分選試劑盒
- 新產(chǎn)品
- 聯(lián)系我們
Duvelisib (IPI-145)
別名: INK1197
Duvelisib (IPI-145, INK1197) 是一種新型選擇性PI3K δ/γ抑制劑，在無(wú)細(xì)胞試驗(yàn)中Ki和IC50分別為 23 pM/243 pM 和 1 nM/50 nM，對(duì) PI3K δ/γ 的選擇性比對(duì)其它蛋白激酶高。Phase 3。
Duvelisib (IPI-145) Chemical Structure
CAS: 1201438-56-3
產(chǎn)品質(zhì)控
批次：
純度：
99.96%
99.96
Duvelisib (IPI-145)相關(guān)產(chǎn)品
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類(lèi)型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| 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(diǎn)擊查看更多細(xì)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(wú)細(xì)胞試驗(yàn)中Ki和IC50分別為 23 pM/243 pM 和 1 nM/50 nM，對(duì) PI3K δ/γ 的選擇性比對(duì)其它蛋白激酶高。Phase 3。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | IPI-145抑制鼠/人類(lèi) B細(xì)胞增殖，EC50 為0.5 nM/0.5 nM，也抑制人類(lèi)T細(xì)胞增殖，EC50為9.5 nM。[1] |
|||
|---|---|---|---|---|
| 實(shí)驗(yàn)圖片 | 檢測(cè)方法 | 檢測(cè)指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | PI3Kγ / PI3Kδ p-AKT / AKT / p-MAPK / MAPK |
|
29522278 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)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(dòng)力學(xué), 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(dǎo)的關(guān)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(hù)關(guān)節(jié)骨和軟骨。IPI-145 (10 mg/kg,QD)有效作用于大鼠佐劑性多關(guān)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(xué)信息&溶解度
| 分子量 | 416.86 | 分子式 | C22H17ClN6O |
| CAS號(hào) | 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(chǔ)存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 83 mg/mL ( (199.1 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | |||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)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(guò)該批次藥物DMSO溶解度，請(qǐng)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(jìn)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。
技術(shù)支持
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* 必填項(xiàng)
常見(jiàn)問(wèn)題及建議解決方法
問(wèn)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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