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Buparlisib (BKM120)
別名: NVP-BKM120 中文名稱：布帕尼西
Buparlisib (BKM120, NVP-BKM120) 是一種選擇性 PI3K 抑制劑，在無細胞試驗中作用于p110α/β/δ/γ的IC50分別為 52 nM/166 nM/116 nM/262 nM。對 VPS34，mTOR，DNAPK 的作用效果下降，而對 PI4Kβ幾乎沒有活性。Buparlisib 可誘導凋亡。Phase 2。
Buparlisib (BKM120) Chemical Structure
CAS: 944396-07-0
產品質控
批次：
純度：
99.93%
99.93
Buparlisib (BKM120)相關產品
相關信號通路圖
細胞實驗數據示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| MDA-MB-361 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| ZR-75-30 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| EFM-19 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| HCC1500 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| MDA-MB-134 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| MDA-MB-175 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| LNZ308 | Function Assay | 5 μM | 24 h | Inhibits phosphorylation of AKT | 24741074 |
| LN18 | Function Assay | 5 μM | 24 h | Inhibits phosphorylation of AKT | 24741074 |
| U87 | Growth Inhibition Assay | 20 μM | 72 h | IC50<5 μM | 24741074 |
| T98G | Growth Inhibition Assay | 20 μM | 72 h | IC50<5 μM | 24741074 |
| LNZ308 | Growth Inhibition Assay | 20 μM | 72 h | IC50<5 μM | 24741074 |
| LN229 | Growth Inhibition Assay | 20 μM | 72 h | IC50<5 μM | 24741074 |
| LN18 | Growth Inhibition Assay | 20 μM | 72 h | IC50<5 μM | 24741074 |
| SJSA-1 | Growth Inhibition Assay | 50 μM | 48 h | Inhibits cell viability | 24727660 |
| MG-63 | Growth Inhibition Assay | 50 μM | 48 h | Inhibits cell viability | 24727660 |
| Saos-2 | Growth Inhibition Assay | 50 μM | 48 h | Inhibits cell viability | 24727660 |
| SJSA-1 | Function Assay | 50 μM | 48 h | Inhibits matrix metalloproteinase-2 expression | 24727660 |
| MG-63 | Function Assay | 50 μM | 48 h | Inhibits matrix metalloproteinase-2 expression | 24727660 |
| Saos-2 | Function Assay | 50 μM | 48 h | Inhibits matrix metalloproteinase-2 expression | 24727660 |
| SJSA-1 | Function Assay | 50 μM | 48 h | Inhibits cell invasion | 24727660 |
| MG-63 | Function Assay | 50 μM | 48 h | Inhibits cell invasion | 24727660 |
| Saos-2 | Function Assay | 50 μM | 48 h | Inhibits cell invasion | 24727660 |
| U87 | Function Assay | 5 μM | 24 h | Reduces oxygen consumption | 24631147 |
| HCT116 | Function Assay | 5 μM | 24 h | Reduces oxygen consumption | 24631147 |
| EMT6 | Function Assay | 5 μM | 24 h | Reduces oxygen consumption | 24631147 |
| FaDu | Function Assay | 5 μM | 24 h | Reduces oxygen consumption | 24631147 |
| GBM | Apoptosis Assay | 2μM | 48h | induced higher levels of apoptosis, and decreased cell viability | 24500492 |
| BON | Apoptosis Assay | 1-5μM | 24h | increases apoptosis | 24443523 |
| BON | Growth Inhibition Assay | 1-5μM | 72h | decreases cell proliferation | 24443523 |
| H1975 | Apoptosis Assay | 2μM | 24h | increases apoptosis rate significantly | 24337846 |
| H1975 | Growth Inhibition Assay | 0.3-9.6μM | 72h | IC50=1.385μM | 24337846 |
| T-ALL | Apoptosis Assay | between 1.4 and 5.3 mM at 24h and 0.9 and 5.5 mM at 48h in different cell line | 24 or 48h | affects the PI3K pathway in T-ALL cell lines | 24310736 |
| BCR-ABL | Growth Inhibition Assay | 0.25-10μM | 4d | significantly inhibit cell proliferation | 24244612 |
| LC-1/SQSF | Function Assay | 3μM | 24h | decrease NRF2 protein level | 23980093 |
| Primary CLL cells | Cytotoxic Assay | 2μM | 24h | induces cell cytotoxicity | 23850807 |
| Primary CLL cells | Kinase Assay | 2μM | 30min | decreased PI3K activity | 23850807 |
| Primary CLL cells | Apoptosis Assay | 1-10μM | 48h | induces apoptosis in CLL cells independent of prognostic markers | 23850807 |
| human NSCLC cell lines | Apoptosis Assay | 0.125-4μM | 24h | IC50s ranges from 0.4-2μM | 23562472 |
| Huh7 | Kinase Assay | 1μM | 48h | signi?cantly reduces phosphorylation of Akt | 23489999 |
| human HCC cell lines | Cell viability assay | 0.005-1μM | 48h | IC50=1μM | 23489999 |
| 786-0 | Growth Inhibition Assay | 1-20μM | 72h | IC50＜1μM | 23479136 |
| SK-HEP1 | Growth Inhibition Assay | 1-20μM | 72h | IC50＜1μM | 23479136 |
| primary B-CLL lymphocytes | Kinase Assay | IC50 for each primary cell line | 24h | inhibits p70S6K & 4E-BP1 expression | 23238639 |
| primary B-CLL lymphocytes | Apoptosis Assay | IC50 for each primary cell line | 24h | IC50＜3μM for all patients | 23238639 |
| MEC2 | Cytotoxicity assay | 0.2-20μM | 72h | IC50=0.7μM | 23238639 |
| EHEB | Cytotoxicity assay | 0.2-20μM | 72h | IC50=0.7μM | 23238639 |
| JVM2 | Cytotoxicity assay | 0.2-20μM | 72h | IC50=0.9μM | 23238639 |
| human NSCLC | Kinase Assay | 1μM | 24h | inhibits the Akt/mTOR signaling pathway at 3h after treatment | 22781393 |
| human NSCLC | Growth Inhibition Assay | 0.5-2μM | 72h | IC50=1μM | 22781393 |
| Y1 cell line | Growth Inhibition Assay | 0.1μM/1μM | 24h | inhibits 60％ cell viability in Myc-Sctr-transfected cells | 22692904 |
| MCF7-myr-Akt | Growth Inhibition Assay | GI50=299±68nM，LD50＞10,000nM | 72h | GI50=299±68nM，LD50＞10,000nM | 22653967 |
| PIK3CA-mutant MCF7 | Kinase Assay | IC50=114±3nM | 72h | IC50=114±3nM in reducing Akt phosphorylation levels | 22653967 |
| PIK3CA-mutant MCF7 | Growth Inhibition Assay | GI50=160±91nM，LD50=980±273nM | 72h | GI50=160±91nM，LD50=980±273nM | 22653967 |
| HT-29 and HCT-116 | Caspase assay | 5μM | 24h | induces caspase activity | 22543857 |
| HCT-116/HT-29/MKN-45 | Apoptosis Assay | 2μM | 48h | shift in G2 phase | 22543857 |
| gastric cancer cell lines | Growth Inhibition Assay | 0-10μM | 72h | IC50=2-5μM | 22543857 |
| colon cancer cell lines | Growth Inhibition Assay | 0-10μM | 72h | IC50=1μM | 22543857 |
| ARP-1 | Apoptosis Assay | 10μM | 24h | induces MM cell apoptosis through caspase activation | 22207485 |
| MM cell lines | Growth Inhibition Assay | 10μM | 24h | IC50 varies among different cell lines in time and dose dependence | 22207485 |
| U87 | Apoptosis Assay | 2μM | 72h | induces cell apoptosis and cleaved PARP and caspase-3 | 22065080 |
| T-47D | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| SK-BR-3 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| UACC-732 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| BT-474 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| HCC202 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| MCF7 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| MDA-MB-415 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| MDA-MB-453 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| ZR-75-1 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| HCC38 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| HCC1419 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| UACC-812 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| HCC1187 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| KPL-1 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| SUM-225 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| EFM-192A | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| JIMT-1 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| HCC1143 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| HCC2218 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| MDA-MB-468 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| BT-20 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| MDA-MB-435 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| BT-549 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| HCC1806 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| HCC1937 | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| Hs578T | Growth Inhibition Assay | 1 μM | 5 d | IC50<1 μM | 24879796 |
| Huh7 | Function Assay | 1 μM | 1 h | Inhibits phosphorylation of AKT at Ser474 | 25004403 |
| BNL | Function Assay | 1 μM | 1 h | Inhibits phosphorylation of S6 | 25004403 |
| BON-1 | Growth Inhibition Assay | 500 nM | 10 d | Inhibits cell growth | 25026292 |
| BON-1 | Function Assay | 500 nM | 4 h | Inhibits phosphorylation of AKT at Thr308 and Ser473 | 25026292 |
| QGP-1 | Function Assay | 500 nM | 4 h | Inhibits phosphorylation of AKT at Thr308 and Ser473 | 25026292 |
| HCT-15 | Apotosis Assay | 10 μM | 48 h | Induces apoptosis in HCT-15 cells harbouring PIK3CA hotspot mutation | 25152245 |
| HCT-116 | Apotosis Assay | 10 μM | 48 h | Induces apoptosis in HCT-116 cells harbouring PIK3CA hotspot mutation | 25152245 |
| NCI-H460 | Apotosis Assay | 10 μM | 48 h | Induces apoptosis in NCI-H460 cells harbouring PIK3CA hotspot mutation | 25152245 |
| SKOV-3 | Apotosis Assay | 10 μM | 48 h | Induces apoptosis in SKOV-3 cells harbouring PIK3CA hotspot mutation | 25152245 |
| BSY-1 | Apotosis Assay | 10 μM | 48 h | Induces apoptosis in BSY-1 cells harbouring PIK3CA hotspot mutation | 25152245 |
| MKN-1 | Apotosis Assay | 10 μM | 48 h | Induces apoptosis in MKN-1 cells harbouring PIK3CA hotspot mutation | 25152245 |
| NCI-H522 | Apotosis Assay | 10 μM | 48 h | Induces apoptosis | 25152245 |
| OVCAR-3 | Apotosis Assay | 10 μM | 48 h | Induces apoptosis | 25152245 |
| HBC-5 | Apotosis Assay | 10 μM | 48 h | Induces apoptosis | 25152245 |
| RXF-631L | Apotosis Assay | 10 μM | 48 h | Induces apoptosis | 25152245 |
| MKN-45 | Apotosis Assay | 10 μM | 48 h | Induces apoptosis | 25152245 |
| A549 | Function Assay | 500 nM | 48 h | Inhibits Akt activation | 25937299 |
| A549 | Growth Inhibition Assay | 1 μM | 72 h | Inhibits cell growth | 25937299 |
| H522 | Growth Inhibition Assay | 1 μM | 72 h | Inhibits cell growth | 25937299 |
| SKMES-1 | Cytotoxic Assay | 1 μM | 72 h | Induces cell death | 26013318 |
| HCT116 | Function assay | 10 uM | 1 hr | Inhibition of PI3K/Akt in human HCT116 cells assessed as Akt phosphorylation at 10 uM after 1 hr by Western blotting analysis | 25765909 |
| A2058 melanoma | Cell cycle assay | 5 uM | 24 hrs | Cell cycle arrest in human A2058 melanoma cells assessed as accumulation at SubG1 phase at 5 uM after 24 hrs by propidium iodide staining based FACS analysis | 28829592 |
| A2058 melanoma | Cell cycle assay | 5 uM | 24 hrs | Cell cycle arrest in human A2058 melanoma cells assessed as accumulation at G2/M phase at 5 uM after 24 hrs by propidium iodide staining based FACS analysis | 28829592 |
| SKOV3 | Cell cycle assay | 2 uM | 24 hrs | Cell cycle arrest in human SKOV3 cells assessed as accumulation at G2/M phase at 2 uM after 24 hrs by propidium iodide staining based FACS analysis | 28829592 |
| SKOV3 | Cell cycle assay | 2 uM | 24 hrs | Cell cycle arrest in human SKOV3 cells assessed as accumulation at SubG1 phase at 2 uM after 24 hrs by propidium iodide staining based FACS analysis | 28829592 |
| HT-29 | Cell cycle assay | 0.111 to 3 uM | 24 hrs | Cell cycle arrest in human HT-29 cells assessed as accumulation at G2/M phase at 0.111 to 3 uM after 24 hrs by propidium iodide staining based flow cytometry | 30034607 |
| LNCaP | Function Assay | 1 μM | Suppresses p-AKT levels | 25360799 | |
| LNCaP95 | Function Assay | 1 μM | Suppresses p-AKT levels | 25360799 | |
| H596 | Function Assay | 1 μM | Impairs cell migration | 26013318 | |
| HCC2450 | Function Assay | 1 μM | Impairs cell invasion | 26013318 | |
| SNU-719 | Growth Inhibition Assay | 72h | IC50=3.037±0.032μM | 22159814 | |
| SNU-620 | Growth Inhibition Assay | 72h | IC50=2.939±0.001μM | 22159814 | |
| SNU-484 | Growth Inhibition Assay | 72h | IC50=1.728±0.045μM | 22159814 | |
| SNU-16 | Growth Inhibition Assay | 72h | IC50=1.573±0.001μM | 22159814 | |
| SNU-638 | Growth Inhibition Assay | 72h | IC50=2.282±0.053μM | 22159814 | |
| SNU-5 | Growth Inhibition Assay | 72h | IC50=1.351±0.091μM | 22159814 | |
| SNU-216 | Growth Inhibition Assay | 72h | IC50=2.692±0.082μM | 22159814 | |
| AGS | Growth Inhibition Assay | 72h | IC50=1.714±0.117μM | 22159814 | |
| SNU-668 | Growth Inhibition Assay | 72h | IC50=1.579±0.074μM | 22159814 | |
| SNU-1 | Growth Inhibition Assay | 72h | IC50=1.082±0.028μM | 22159814 | |
| SNU-601 | Growth Inhibition Assay | 72h | IC50=0.816±0.063μM | 22159814 | |
| glioma cell lines | Growth Inhibition Assay | 72h | IC50=1-2μM | 22065080 | |
| MCF7 | Cytotoxic Assay | 72 h | Cytotoxicity against human MCF7 cells expressing PI3Kalpha E545K mutant with GI50 of 0.000158 μM | 24900266 | |
| DU145 | Cytotoxic Assay | 72 h | Cytotoxicity against human DU145 cells expressing LKB1 mutant with GI50 of 0.000435 μM | 24900266 | |
| A2780 | Cytotoxic Assay | 72 h | Cytotoxicity against PTEN-deficient human A2780 cells with GI50 of 0.000635 μM | 24900266 | |
| U87MG | Cytotoxic Assay | 72 h | Cytotoxicity against PTEN-deficient human U87MG cells with GI50 of 0.000698 μM | 24900266 | |
| A2780 | Function Assay | 1 h | Inhibition of PI3K-mediated AKT Ser473 phosphorylation with EC50 of 0.055 μM | 24900266 | |
| DU145 | Function Assay | 1 h | Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human DU145 cells harboring LKB1 mutation with EC50 of 0.073 μM | 24900266 | |
| A2780 | Function Assay | 1 h | Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human A2780 cells with EC50 of 0.074 μM | 24900266 | |
| MCF7 | Function Assay | 1 h | Inhibition of PI3Kalpha E545K mutant-mediated AKT Ser473 phosphorylation with EC50 of 0.1 μM | 24900266 | |
| U87MG | Function Assay | 1 h | Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human U87MG cells with EC50 of 0.13 μM | 24900266 | |
| A2780 | Growth Inhibition Assay | 72 h | EC50=0.52 μM | 24900266 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 0.48 μM. | 25765909 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 1 μM. | 25765909 | |
| U87MG | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay, IC50 = 1.64 μM. | 25765909 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 2.07 μM. | 25765909 | |
| HeLa | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50 = 4.34 μM. | 25765909 | |
| MDA-MB-231 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 1.88 μM. | 29107429 | |
| PC3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50 = 5.34 μM. | 29107429 | |
| T47D | Cytotoxicity assay | 72 hrs | Cytotoxicity against human T47D cells after 72 hrs by MTT assay, IC50 = 6.92 μM. | 29107429 | |
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 11.05 μM. | 29107429 | |
| Sf21 | Function assay | 1 hr | Inhibition of recombinant human full-length N-terminal His6-tagged p110delta/recombinant human full length p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 1 hr by Alexa633 Tracer-based fluorescence polar, IC50 = 0.125 μM. | 30034607 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay, IC50 = 0.206 μM. | 30034607 | |
| Sf21 | Function assay | 1 hr | Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/recombinant human full length p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 1 hr by Alexa633 Tracer-based fluorescence polari, IC50 = 0.234 μM. | 30034607 | |
| T47D | Antiproliferative assay | 72 hrs | Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay, IC50 = 0.286 μM. | 30034607 | |
| PC3 | Function assay | 2 hrs | Inhibition of PI3K in human PC3 cells assessed as reduction in AKT phosphorylation at Ser473 measured after 2 hrs by fluorescence assay, IC50 = 0.365 μM. | 30034607 | |
| A2058 | Function assay | 1 hr | Inhibition of TORC2 in human A2058 cells assessed as decrease in PKB/Akt phosphorylation at Ser473 after 1 hr by Western blot analysis, IC50 = 0.416 μM. | 30359003 | |
| A2058 | Function assay | 1 hr | Inhibition of TORC1 in human A2058 cells assessed as decrease in S6 phosphorylation at Ser235/236 after 1 hr by Western blot analysis, IC50 = 0.553 μM. | 30359003 | |
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| insect | Function assay | Inhibition of recombinant human His-tagged p85alpha/p110alpha E545K mutant expressed in insect cells, IC50 = 0.011 μM. | 30034607 | ||
| insect | Function assay | Inhibition of recombinant human His-tagged p85alpha/p110alpha E542K mutant expressed in insect cells, IC50 = 0.029 μM. | 30034607 | ||
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生物活性
| 產品描述 | Buparlisib (BKM120, NVP-BKM120) 是一種選擇性 PI3K 抑制劑，在無細胞試驗中作用于p110α/β/δ/γ的IC50分別為 52 nM/166 nM/116 nM/262 nM。對 VPS34，mTOR，DNAPK 的作用效果下降，而對 PI4Kβ幾乎沒有活性。Buparlisib 可誘導凋亡。Phase 2。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | BKM120是可用于口服的生物有效的PI3K抑制劑。 | |||||||||||
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | BKM120作用于解除PI3K調節(jié)的細胞系，包括A2780, U87MG, MCF7和DU145時，具有抗增殖活性，GI50為0.1-0.7 nM。[1] BKM120誘導多發(fā)性骨髓瘤細胞(ARP1, ARK, MM.1S, MM1.R和U266)凋亡，導致G1期細胞增多，S期細胞減少。BKM120誘導CD138+原代MM 細胞凋亡，且作用于CD138?基質細胞時毒性較低。BKM120可引起B(yǎng)imS的上調和XIAP的下調。[2]BKM120作用于人類胃癌細胞系，降低mTOR下游信號，具有抗增殖活性。BKM120作用于KRAS突變的胃癌細胞系，可以增強p-ERK或 p-STAT3。BKM120 和STAT3阻斷劑聯(lián)用, 作用于含突變KRAS的細胞，誘導凋亡，具有協(xié)同效應，但是作用于KRAS野生型細胞沒有這種效果。[3]BKM120主要通過Aurora B激酶調節(jié)有絲分裂崩壞。[4] | |||
|---|---|---|---|---|
| 激酶實驗 | PI3K 生化實驗(ATP 消耗實驗) | |||
| BKM120溶于DMSO中，按每孔1.25 μL直接加到黑色384孔板上。開始反應, 25 μL 10nM PI3K和5 μg/mL 1-α-磷酸肌醇(PI)加到實驗 buffer (10 mM Tris pH 為7.5, 5 mM MgCl2, 20 mM NaCl, 1 mM DTT，及0.05% CHAPS)，然后加到每孔中，隨后在實驗buffer中加入25 μL 2 μM ATP。反應進行直到50% ATP被消耗，然后加入25 μL KinaseGlo溶液終止反應。終止的反應溫育5分鐘，然后通過熒光測定殘留的ATP。 | ||||
| 細胞實驗 | 細胞系 | A2780細 胞 | ||
| 濃度 | 0-6.6 μM | |||
| 孵育時間 | 3天 | |||
| 方法 | A2780細胞培養(yǎng)在含10% FBS,L-谷氨酸,丙酮酸鈉和抗生素的DMEM培養(yǎng)基上。細胞按每孔103個細胞的密度接種在相同培養(yǎng)基上，溫育3到5小時。稀釋溶于20 mM DMSO中的BKM120。2 μL稀釋的BKM120溶液加到細胞培養(yǎng)基上, (濃度為0-6.6 μM)。等體積(100 μL)溶液加到96孔板中，在37oC下溫育3天。使用Trilux讀取熒光值而測定抑制細胞增殖的效果 | |||
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | p-MET / MET p-STAT3 / STAT3 / p-ERK / ERK / p-S6 p-ERK / ERK / LC3 Nuclear NF-κB p65 / NF-κB p65 p-FOXO3a (S253) / FOXO3a p-AKT (T308) / p-AKT (S473) / AKT |
|
29928341 | |
| Immunofluorescence | FOXO3a |
|
28036259 | |
| Growth inhibition assay | Cell viability |
|
26673665 | |
| 體內研究(In Vivo) | ||
| 體內研究活性 | BKM120按30, 60, 或100 mg/kg劑量作用于A2780移植瘤，完全抑制pAKTser473。BKM120按 30和 60 mg/kg劑量作用于U87MG神經膠質瘤模型，顯示抗癌活性。[1]BKM120每天按5μM/kg劑量處理具有持久生命力的ARP1 SCID鼠模型，導致腫瘤體積和K鏈水平明顯降低。[2] | |
|---|---|---|
| 動物實驗 | Animal Models | 攜帶U87MG 和A2780移植瘤的雌性裸鼠 |
| Dosages | ~60 mg/kg | |
| Administration | 每天口服處理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04338399 | Active not recruiting | Head and Neck Cancer |
Adlai Nortye Biopharma Co. Ltd. |
December 12 2020 | Phase 3 |
| NCT02614508 | Terminated | Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma |
Emory University|Novartis |
January 2016 | Phase 1 |
| NCT01613677 | Withdrawn | Treatment for Metastatic or Locally Advanced Cervical Cancer |
Novartis Pharmaceuticals|Novartis |
November 2015 | Phase 2 |
化學信息&溶解度
| 分子量 | 410.39 | 分子式 | C18H21F3N6O2 |
| CAS號 | 944396-07-0 | SDF | Download Buparlisib (BKM120) SDF |
| Smiles | C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 82 mg/mL ( (199.8 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 82 mg/mL (199.8 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內溶解度 現配現用，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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