연구용
Buparlisib (BKM120) PI3K 억제제
제품 번호S2247
화학 구조
분자량: 410.39
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품질 관리
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순도:
99.94%
99.94
세포 배양, 처리 및 작업 농도
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| glioma cell lines | Growth Inhibition Assay | 72h | IC50=1-2μM | 22065080 | ||
| U87 | Apoptosis Assay | 2μM | 72h | induces cell apoptosis and cleaved PARP and caspase-3 | 22065080 | |
| SNU-601 | Growth Inhibition Assay | 72h | DMSO | IC50=0.816±0.063μM | 22159814 | |
| SNU-1 | Growth Inhibition Assay | 72h | DMSO | IC50=1.082±0.028μM | 22159814 | |
| SNU-668 | Growth Inhibition Assay | 72h | DMSO | IC50=1.579±0.074μM | 22159814 | |
| AGS | Growth Inhibition Assay | 72h | DMSO | IC50=1.714±0.117μM | 22159814 | |
| SNU-216 | Growth Inhibition Assay | 72h | DMSO | IC50=2.692±0.082μM | 22159814 | |
| SNU-5 | Growth Inhibition Assay | 72h | DMSO | IC50=1.351±0.091μM | 22159814 | |
| SNU-638 | Growth Inhibition Assay | 72h | DMSO | IC50=2.282±0.053μM | 22159814 | |
| SNU-16 | Growth Inhibition Assay | 72h | DMSO | IC50=1.573±0.001μM | 22159814 | |
| SNU-484 | Growth Inhibition Assay | 72h | DMSO | IC50=1.728±0.045μM | 22159814 | |
| SNU-620 | Growth Inhibition Assay | 72h | DMSO | IC50=2.939±0.001μM | 22159814 | |
| SNU-719 | Growth Inhibition Assay | 72h | DMSO | IC50=3.037±0.032μM | 22159814 | |
| MM cell lines | Growth Inhibition Assay | 10μM | 24h | DMSO | IC50 varies among different cell lines in time and dose dependence | 22207485 |
| ARP-1 | Apoptosis Assay | 10μM | 24h | DMSO | induces MM cell apoptosis through caspase activation | 22207485 |
| colon cancer cell lines | Growth Inhibition Assay | 0-10μM | 72h | DMSO | IC50=1μM | 22543857 |
| gastric cancer cell lines | Growth Inhibition Assay | 0-10μM | 72h | DMSO | IC50=2-5μM | 22543857 |
| HCT-116/HT-29/MKN-45 | Apoptosis Assay | 2μM | 48h | shift in G2 phase | 22543857 | |
| HT-29 and HCT-116 | Caspase assay | 5μM | 24h | induces caspase activity | 22543857 | |
| PIK3CA-mutant MCF7 | Growth Inhibition Assay | GI50=160±91nM，LD50=980±273nM | 72h | GI50=160±91nM，LD50=980±273nM | 22653967 | |
| PIK3CA-mutant MCF7 | Kinase Assay | IC50=114±3nM | 72h | IC50=114±3nM in reducing Akt phosphorylation levels | 22653967 | |
| MCF7-myr-Akt | Growth Inhibition Assay | GI50=299±68nM，LD50＞10,000nM | 72h | GI50=299±68nM，LD50＞10,000nM | 22653967 | |
| Y1 cell line | Growth Inhibition Assay | 0.1μM/1μM | 24h | DMSO | inhibits 60％ cell viability in Myc-Sctr-transfected cells | 22692904 |
| human NSCLC | Growth Inhibition Assay | 0.5-2μM | 72h | IC50=1μM | 22781393 | |
| human NSCLC | Kinase Assay | 1μM | 24h | inhibits the Akt/mTOR signaling pathway at 3h after treatment | 22781393 | |
| JVM2 | Cytotoxicity assay | 0.2-20μM | 72h | DMSO | IC50=0.9μM | 23238639 |
| EHEB | Cytotoxicity assay | 0.2-20μM | 72h | DMSO | IC50=0.7μM | 23238639 |
| MEC2 | Cytotoxicity assay | 0.2-20μM | 72h | DMSO | IC50=0.7μM | 23238639 |
| primary B-CLL lymphocytes | Apoptosis Assay | IC50 for each primary cell line | 24h | DMSO | IC50＜3μM for all patients | 23238639 |
| primary B-CLL lymphocytes | Kinase Assay | IC50 for each primary cell line | 24h | inhibits p70S6K & 4E-BP1 expression | 23238639 | |
| SK-HEP1 | Growth Inhibition Assay | 1-20μM | 72h | DMSO | IC50＜1μM | 23479136 |
| 786-0 | Growth Inhibition Assay | 1-20μM | 72h | DMSO | IC50＜1μM | 23479136 |
| human HCC cell lines | Cell viability assay | 0.005-1μM | 48h | IC50=1μM | 23489999 | |
| Huh7 | Kinase Assay | 1μM | 48h | significantly reduces phosphorylation of Akt | 23489999 | |
| human NSCLC cell lines | Apoptosis Assay | 0.125-4μM | 24h | DMSO | IC50s ranges from 0.4-2μM | 23562472 |
| Primary CLL cells | Apoptosis Assay | 1-10μM | 48h | induces apoptosis in CLL cells independent of prognostic markers | 23850807 | |
| Primary CLL cells | Kinase Assay | 2μM | 30min | decreased PI3K activity | 23850807 | |
| Primary CLL cells | Cytotoxic Assay | 2μM | 24h | induces cell cytotoxicity | 23850807 | |
| LC-1/SQSF | Function Assay | 3μM | 24h | DMSO | decrease NRF2 protein level | 23980093 |
| BCR-ABL | Growth Inhibition Assay | 0.25-10μM | 4d | significantly inhibit cell proliferation | 24244612 | |
| 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 | DMSO | affects the PI3K pathway in T-ALL cell lines | 24310736 |
| H1975 | Growth Inhibition Assay | 0.3-9.6μM | 72h | DMSO | IC50=1.385μM | 24337846 |
| H1975 | Apoptosis Assay | 2μM | 24h | DMSO | increases apoptosis rate significantly | 24337846 |
| BON | Growth Inhibition Assay | 1-5μM | 72h | decreases cell proliferation | 24443523 | |
| BON | Apoptosis Assay | 1-5μM | 24h | increases apoptosis | 24443523 | |
| GBM | Apoptosis Assay | 2μM | 48h | DMSO | induced higher levels of apoptosis, and decreased cell viability | 24500492 |
| FaDu | Function Assay | 5 μM | 24 h | DMSO | Reduces oxygen consumption | 24631147 |
| EMT6 | Function Assay | 5 μM | 24 h | DMSO | Reduces oxygen consumption | 24631147 |
| HCT116 | Function Assay | 5 μM | 24 h | DMSO | Reduces oxygen consumption | 24631147 |
| U87 | Function Assay | 5 μM | 24 h | DMSO | Reduces oxygen consumption | 24631147 |
| Saos-2 | Function Assay | 50 μM | 48 h | Inhibits cell invasion | 24727660 | |
| MG-63 | Function Assay | 50 μM | 48 h | Inhibits cell invasion | 24727660 | |
| SJSA-1 | Function Assay | 50 μM | 48 h | Inhibits cell invasion | 24727660 | |
| Saos-2 | 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 | |
| SJSA-1 | Function Assay | 50 μM | 48 h | Inhibits matrix metalloproteinase-2 expression | 24727660 | |
| Saos-2 | Growth Inhibition Assay | 50 μM | 48 h | Inhibits cell viability | 24727660 | |
| MG-63 | Growth Inhibition Assay | 50 μM | 48 h | Inhibits cell viability | 24727660 | |
| SJSA-1 | Growth Inhibition Assay | 50 μM | 48 h | Inhibits cell viability | 24727660 | |
| LN18 | Growth Inhibition Assay | 20 μM | 72 h | DMSO | IC50<5 μM | 24741074 |
| LN229 | Growth Inhibition Assay | 20 μM | 72 h | DMSO | IC50<5 μM | 24741074 |
| LNZ308 | Growth Inhibition Assay | 20 μM | 72 h | DMSO | IC50<5 μM | 24741074 |
| T98G | Growth Inhibition Assay | 20 μM | 72 h | DMSO | IC50<5 μM | 24741074 |
| U87 | Growth Inhibition Assay | 20 μM | 72 h | DMSO | IC50<5 μM | 24741074 |
| LN18 | Function Assay | 5 μM | 24 h | DMSO | Inhibits phosphorylation of AKT | 24741074 |
| LNZ308 | Function Assay | 5 μM | 24 h | DMSO | Inhibits phosphorylation of AKT | 24741074 |
| MDA-MB-175 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| MDA-MB-134 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| HCC1500 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| EFM-19 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| ZR-75-30 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| MDA-MB-361 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| T-47D | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| SK-BR-3 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| UACC-732 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| BT-474 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| HCC202 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| MCF7 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| MDA-MB-415 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| MDA-MB-453 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| ZR-75-1 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| HCC38 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| HCC1419 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| UACC-812 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| HCC1187 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| KPL-1 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| SUM-225 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| EFM-192A | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| JIMT-1 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| HCC1143 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| HCC2218 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| MDA-MB-468 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| BT-20 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| MDA-MB-435 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| BT-549 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| HCC1806 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| HCC1937 | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| Hs578T | Growth Inhibition Assay | 1 μM | 5 d | DMSO | IC50<1 μM | 24879796 |
| MCF7 | Cytotoxic Assay | 72 h | DMSO | Cytotoxicity against human MCF7 cells expressing PI3Kalpha E545K mutant with GI50 of 0.000158 μM | 24900266 | |
| DU145 | Cytotoxic Assay | 72 h | DMSO | Cytotoxicity against human DU145 cells expressing LKB1 mutant with GI50 of 0.000435 μM | 24900266 | |
| A2780 | Cytotoxic Assay | 72 h | DMSO | Cytotoxicity against PTEN-deficient human A2780 cells with GI50 of 0.000635 μM | 24900266 | |
| U87MG | Cytotoxic Assay | 72 h | DMSO | Cytotoxicity against PTEN-deficient human U87MG cells with GI50 of 0.000698 μM | 24900266 | |
| A2780 | Function Assay | 1 h | DMSO | Inhibition of PI3K-mediated AKT Ser473 phosphorylation with EC50 of 0.055 μM | 24900266 | |
| DU145 | Function Assay | 1 h | DMSO | 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 | DMSO | 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 | DMSO | Inhibition of PI3Kalpha E545K mutant-mediated AKT Ser473 phosphorylation with EC50 of 0.1 μM | 24900266 | |
| U87MG | Function Assay | 1 h | DMSO | 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 | DMSO | EC50=0.52 μM | 24900266 | |
| Huh7 | Function Assay | 1 μM | 1 h | DMSO | Inhibits phosphorylation of AKT at Ser474 | 25004403 |
| BNL | Function Assay | 1 μM | 1 h | DMSO | Inhibits phosphorylation of S6 | 25004403 |
| BON-1 | Growth Inhibition Assay | 500 nM | 10 d | DMSO | Inhibits cell growth | 25026292 |
| BON-1 | Function Assay | 500 nM | 4 h | DMSO | Inhibits phosphorylation of AKT at Thr308 and Ser473 | 25026292 |
| QGP-1 | Function Assay | 500 nM | 4 h | DMSO | Inhibits phosphorylation of AKT at Thr308 and Ser473 | 25026292 |
| HCT-15 | Apotosis Assay | 10 μM | 48 h | DMSO | Induces apoptosis in HCT-15 cells harbouring PIK3CA hotspot mutation | 25152245 |
| HCT-116 | Apotosis Assay | 10 μM | 48 h | DMSO | Induces apoptosis in HCT-116 cells harbouring PIK3CA hotspot mutation | 25152245 |
| NCI-H460 | Apotosis Assay | 10 μM | 48 h | DMSO | Induces apoptosis in NCI-H460 cells harbouring PIK3CA hotspot mutation | 25152245 |
| SKOV-3 | Apotosis Assay | 10 μM | 48 h | DMSO | Induces apoptosis in SKOV-3 cells harbouring PIK3CA hotspot mutation | 25152245 |
| BSY-1 | Apotosis Assay | 10 μM | 48 h | DMSO | Induces apoptosis in BSY-1 cells harbouring PIK3CA hotspot mutation | 25152245 |
| MKN-1 | Apotosis Assay | 10 μM | 48 h | DMSO | Induces apoptosis in MKN-1 cells harbouring PIK3CA hotspot mutation | 25152245 |
| NCI-H522 | Apotosis Assay | 10 μM | 48 h | DMSO | Induces apoptosis | 25152245 |
| OVCAR-3 | Apotosis Assay | 10 μM | 48 h | DMSO | Induces apoptosis | 25152245 |
| HBC-5 | Apotosis Assay | 10 μM | 48 h | DMSO | Induces apoptosis | 25152245 |
| RXF-631L | Apotosis Assay | 10 μM | 48 h | DMSO | Induces apoptosis | 25152245 |
| MKN-45 | Apotosis Assay | 10 μM | 48 h | DMSO | Induces apoptosis | 25152245 |
| LNCaP | Function Assay | 1 μM | Suppresses p-AKT levels | 25360799 | ||
| LNCaP95 | Function Assay | 1 μM | Suppresses p-AKT levels | 25360799 | ||
| A549 | Function Assay | 500 nM | 48 h | DMSO | Inhibits Akt activation | 25937299 |
| A549 | Growth Inhibition Assay | 1 μM | 72 h | DMSO | Inhibits cell growth | 25937299 |
| H522 | Growth Inhibition Assay | 1 μM | 72 h | DMSO | Inhibits cell growth | 25937299 |
| SKMES-1 | Cytotoxic Assay | 1 μM | 72 h | Induces cell death | 26013318 | |
| H596 | Function Assay | 1 μM | Impairs cell migration | 26013318 | ||
| HCC2450 | Function Assay | 1 μM | Impairs cell invasion | 26013318 | ||
| 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 | ||
| 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 | |
| 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 | ||
| 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 | |||
| 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 | ||
| 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 | |
| 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 | ||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
화학 정보, 보관 및 안정성
| 분자량 | 410.39 | 화학식 | C18H21F3N6O2 |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 944396-07-0 | SDF 다운로드 | 원액 보관 |
|
|
| 동의어 | NVP-BKM120 | Smiles | C1COCCN1C2=NC(=NC(=C2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4 | ||
용해도
|
In vitro |
DMSO
: 82 mg/mL
(199.8 mM)
Ethanol : 25 mg/mL Water : Insoluble |
몰농도 계산기
희석 계산기
분자량 계산기
|
In vivo |
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생체 내 제형 계산기 (투명한 용액)
1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
mg/kg
g
μL
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
계산 결과:
작업 농도: mg/ml;
DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.
참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.
작용 메커니즘
| Targets/IC50/Ki |
p110α
(Cell-free assay) 52 nM
p110δ
(Cell-free assay) 116 nM
p110β
(Cell-free assay) 166 nM
p110γ
(Cell-free assay) 262 nM
Vps34
(Cell-free assay) 2.4 μM
mTOR
(Cell-free assay) 4.6 μM
|
|---|---|
| 시험관 내(In vitro) |
Buparlisib (BKM120)은 Class III 및 Class IV PI3K 또는 PI4K에 민감하지 않습니다. A2780, U87MG, MCF7 및 DU145를 포함한 PI3K 조절 이상 세포주에 대해 0.1-0.7 nM의 GI50으로 우수한 항증식 활성을 보입니다. 이 화합물은 다발성 골수종 세포(ARP1, ARK, MM.1S, MM1.R 및 U266)의 세포자멸사를 유도하여 G1기 세포를 증가시키고 S기 세포를 감소시킵니다. 또한 CD138+ 원발성 MM 세포의 세포자멸사를 유도했으며 CD138- 기질 세포에 대해 유의하게 낮은 세포독성을 보였습니다. 이 노출은 BimS의 상향 조절과 XIAP의 하향 조절을 유발할 수 있습니다. BKM120은 mTOR 하류 신호 전달을 감소시켜 인간 위암 세포주에서 항증식 활성을 보입니다. KRAS 돌연변이 위암 세포에서 p-ERK 또는 p-STAT3를 증가시킬 수 있습니다. STAT3 차단과 병용 시, 돌연변이 KRAS를 보유한 세포에서 세포자멸사를 유도하여 시너지 효과를 보이지만, KRAS 야생형 세포에서는 그렇지 않습니다. 최근 연구에 따르면, p53 상태에 따라 세포 사멸의 다양한 형태를 보이며, p53 야생형 세포는 세포자멸사성 세포 사멸을 겪고 p53 돌연변이/결실 세포는 유사 분열 재해 세포 사멸을 겪습니다. 주로 Aurora B 키나아제를 통해 유사 분열 재해를 매개합니다.
|
| 키나아제 분석 |
PI3K 생화학적 분석 (ATP 고갈 분석)
|
|
Buparlisib (BKM120)은 DMSO에 용해되어 각 웰당 1.25 µL씩 검은색 384웰 플레이트에 직접 분주됩니다. 반응을 시작하기 위해 25 µL의 10 nM PI3 키나아제와 5 µg/mL의 1-α-포스파티딜이노시톨 (PI)을 분석 버퍼 (10 mM Tris pH 7.5, 5 mM MgCl2, 20 mM NaCl, 1 mM DTT 및 0.05% CHAPS)에 넣은 후, 25 µL의 2 µM ATP를 분석 버퍼에 첨가합니다. 반응은 약 50%의 ATP가 고갈될 때까지 진행되며, 그 후 25 µL의 KinaseGlo 용액을 첨가하여 중단됩니다. 중단된 반응은 5분 동안 배양되며, 남아있는 ATP는 발광을 통해 검출됩니다.
|
|
| 생체 내(In vivo) |
Buparlisib (BKM120)은 각각 30, 60 또는 100 mg/kg 용량에서 A2780 이종이식 종양에서 pAktser473을 완전히 억제하며, 30 및 60 mg/kg 용량에서 U87MG 교모세포종 모델에 대한 항종양 활성도 보입니다. 이 화합물 치료는 ARP1 SCID 마우스 모델에서 5 μM/kg/day−1 용량으로 종양 부피와 순환 인간 카파 사슬 수준을 유의하게 감소시켜 생존 기간을 연장시켰습니다.
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참조 |
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적용 분야
| 방법 | 바이오마커 | 이미지 | 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 |
임상시험 정보
(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| 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 |
기술 지원
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