Celecoxib
别名: SC 58635 中文名称：塞来昔布
Celecoxib是一种选择性COX-2抑制剂，在Sf9细胞中IC50为40 nM。
Celecoxib Chemical Structure
CAS: 169590-42-5
产品质控
批次：
纯度：
99.92%
99.92
Celecoxib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 |
|---|---|---|---|---|---|
| LNCaP | Growth Inhibition Assay | 2/5/10 μM | 96 h | inhibits cell growth significantly combined with atorvastatin | 24296978 |
| CF33 | Function Assay | 10-100 μM | 4-24 h | decreases cells in the S phase and increases cells in G0/G1 arrest | 24503782 |
| CF33 | Growth Inhibition Assay | 10-100 μM | 0-4 d | inhibits cell proliferation in a dose-dependent manner | 24503782 |
| CF33 | Function Assay | 100 μM | 24 h | induces downregulation of COX-2 protein expression | 24503782 |
| OVCAR-3 | Function Assay | 10 µM | 1 h | inhibits paclitaxel-induced Akt phosphorylation | 24520227 |
| OVCAR-3 | Function Assay | 10 µM | 1 h | down-regulates NF-κB activation induced by paclitaxel | 24520227 |
| OVCAR-3 | Function Assay | 10 µM | 1 h | enhances paclitaxel-induced activation of caspase-9 | 24520227 |
| OVCAR-3 | Apoptosis Assay | 10 µM | 1 h | promotes paclitaxel-induced apoptosis | 24520227 |
| LMeC | Function Assay | 20/50 μM | 48 h | induces caspase-3 activation | 24656746 |
| OVCAR-3 | Cell Viability Assay | 10 µM | 1 h | enhances paclitaxel-induced ovarian cancer cell death | 24520227 |
| CMeC-1 | Function Assay | 20/50 μM | 48 h | induces caspase-3 activation | 24656746 |
| LMeC | Function Assay | 20/50 μM | 48 h | decreases the levels of cyclin D1 in a dose-dependent manner | 24656746 |
| CMeC-1 | Function Assay | 20/50 μM | 48 h | decreases the levels of cyclin D1 in a dose-dependent manner | 24656746 |
| LMeC | Function Assay | 20/50 μM | 48 h | induces G1-S arrest | 24656746 |
| CMeC-1 | Function Assay | 20/50 μM | 48 h | induces G1-S arrest | 24656746 |
| LMeC | Cell Viability Assay | 20/50 μM | 48 h | inhibits cell viability in a dose dependent manner | 24656746 |
| CMeC-1 | Cell Viability Assay | 20/50 μM | 48 h | inhibits cell viability in a dose dependent manner | 24656746 |
| LMeC | Function Assay | 20/50 μM | 48 h | decreases the expression of COX-2 protein | 24656746 |
| SGC-7901 | Function Assay | 75/100/125 μM | 24/48/72 h | increases caspase-8 and -9 mRNA expression in both time and dose manner | 24676394 |
| SGC-7901 | Apoptosis Assay | 100 μM | 72 h | induces apoptosis | 24676394 |
| SGC-7901 | Growth Inhibition Assay | 50-125 μM | 24/48/72 h | inhibits cell growth in both time and dose dependent manner | 24676394 |
| SNU-1041 | Function Assay | 0-40 μM | 4 h | up-regulates CHOP after treatment with high concentrations | 24692703 |
| SNU-1041 | Function Assay | 20/30 μM | 4 h | induces expression of CHOP, GRP78 and XBP1 at the RNA level | 24692703 |
| SNU-1041 | Growth Inhibition Assay | 0-40 μM | 48 h | inhibits cell viability in a dose dependent manner | 24692703 |
| CNE-1 | Cytotoxicity Assay | 60 μM | 7 d | enhances radiation cytotoxicity through COX-2-dependent manner | 24854838 |
| C666-1 | Cytotoxicity Assay | 60 μM | 7 d | enhances radiation cytotoxicity through COX-2-dependent manner | 24854838 |
| CNE-2 | Cytotoxicity Assay | 20-80 μM | 24 h | decreases colony formation in a dose-dependent manner | 24854838 |
| CNE-1 | Cytotoxicity Assay | 20-80 μM | 24 h | decreases colony formation in a dose-dependent manner | 24854838 |
| C666-1 | Cytotoxicity Assay | 20-80 μM | 24 h | decreases colony formation in a dose-dependent manner | 24854838 |
| MKN-45 | Function Assay | 10/50/100 μM | 48 h | downregulates the mRNA expression levels of COX-2 and PCNA in a dose dependent manner | 24992958 |
| SGC-7901 | Function Assay | 10/50/100 μM | 48 h | downregulates the mRNA expression levels of COX-2 and PCNA in a dose dependent manner | 24992958 |
| MKN-45 | Growth Inhibition Assay | 10/50/100 μM | 24/48/72 h | inhibits cell growth in both time and dose dependent manner | 24992958 |
| SGC-7901 | Growth Inhibition Assay | 10/50/100 μM | 24/48/72 h | inhibits cell growth in both time and dose dependent manner | 24992958 |
| Hep-2 | Function Assay | 50 μM | 0-48 h | reduces the telomerase activity gradually | 24998564 |
| Hep-2 | Function Assay | 50 μM | 0-48 h | decreases the mRNA expression of hTERT | 24998564 |
| Hep-2 | Apoptosis Assay | 50 μM | 0-48 h | induces apoptosis in a time dependent manner | 24998564 |
| Hep-2 | Growth Inhibition Assay | 30/50/100 μM | 12/24/36/48 h | inhibits cell growth in both time and dose dependent manner | 24998564 |
| HSC3 | Function Assay | 25 μM | 72 h | decreases MMP-2 and MMP-9 proteins | 25198789 |
| HSC3 | Function Assay | 25 μM | 48 h | inhibits HSC3 cell invasion combined with CET | 25198789 |
| HSC3 | Function Assay | 25 μM | 48 h | exhibits significantly reduced migration combined with CET | 25198789 |
| HSC3 | Apoptosis Assay | 25 μM | 48 h | induces apoptosis | 25198789 |
| HSC3 | Cell Viability Assay | 0–40 μM | 48 h | IC50=25.5±1.780 μM | 25198789 |
| HT-29 | Function Assay | 10-50 μM | 6-36 h | induces the expression of COX-2 in both dose and time dependent manner | 25218028 |
| HCT-15 | Function Assay | 10-50 μM | 6-36 h | induces the expression of COX-2 in both dose and time dependent manner | 25218028 |
| SKOV3 | Function Assay | 5/10/15 μM | 1 h | increases the expression of p-AKT and p-ERK in a dose-dependent manner | 25424898 |
| A2780 | Function Assay | 5/10/15 μM | 1 h | increases the expression of p-AKT and p-ERK in a dose-dependent manner | 25424898 |
| SKOV3 | Function Assay | 5/10/15 μM | 48 h | decreases the expression of N-cadherin and Vimentin | 25424898 |
| A2780 | Function Assay | 5/10/15 μM | 48 h | decreases the expression of N-cadherin and Vimentin | 25424898 |
| SKOV3 | Function Assay | 5/10/15 μM | 48 h | elevates the expression of E-cadherin and keratin | 25424898 |
| A2780 | Function Assay | 5/10/15 μM | 48 h | elevates the expression of E-cadherin and keratin | 25424898 |
| SKOV3 | Function Assay | 5/10/15 μM | 48 h | decreases Cox-2 expression in a dose-dependent manner | 25424898 |
| A2780 | Function Assay | 5/10/15 μM | 48 h | decreases Cox-2 expression in a dose-dependent manner | 25424898 |
| MCF7-MX | Function Assay | 0-40 µM | 4-24 h | enhances the effects of TPA on ABCG2 expression | 25587329 |
| MDA-MB-231 | Function Assay | 0-40 µM | 4-24 h | stimulates the expression of ABCG2 up to 4.27 times to control level by 12 h | 25587329 |
| MCF-7 | Function Assay | 0-40 µM | 4-24 h | enhances the effects of TPA on ABCG2 expression | 25587329 |
| MDA-MB-231 | Function Assay | 0-40 µM | 4-24 h | increases COX-2 protein expression in both time and dose dependent manner | 25587329 |
| LNCaP | Apoptosis Assay | 2/5/10 μM | 96 h | induces apoptosis combined with atorvastatin | 24296978 |
| MDA-MB-231 | Growth Inhibition Assay | 1/10 μM | 72 h | enhances calcitriol-induced cell growth inhibition | 25667510 |
| MCF-7 | Growth Inhibition Assay | 1/10 μM | 72 h | enhances calcitriol-induced cell growth inhibition | 25667510 |
| SGC7901 | Function Assay | 40 μM | 8/16/24 h | upregulats Cbl-b expression | 25701378 |
| MGC803 | Function Assay | 40 μM | 8/16/24 h | upregulats Cbl-b expression | 25701378 |
| SGC7901 | Growth Inhibition Assay | 0-60 μM | 72 h | IC50=43.53 ± 5.12 μM | 25701378 |
| MGC803 | Growth Inhibition Assay | 0-60 μM | 72 h | IC50=47.25 ± 6.43 μM | 25701378 |
| HLCZ01 | Function Assay | 40 μM | 24 h | increases TRAIL expression combined with Interferon-α | 25724899 |
| HLCZ01 | Apoptosis Assay | 40 μM | 24 h | enhances apoptosis combined with IFN-α | 25724899 |
| HLCZ01 | Function Assay | 40 μM | 24 h | increases accumulation of G0/G1-phase cells combined with IFN-α | 25724899 |
| HLCZ01 | Growth Inhibition Assay | 0–60 µM | 48 h | inhibits cell growth in a dose dependent manner | 25724899 |
| SACC-83 | Function Assay | 20/40/80 μM | 24 h | upregulats PTEN partially by inhibiting Sp1, and activates PTEN and inactivates AKT | 25770423 |
| HeLa | Function Assay | 20/40/80 μM | 24 h | upregulats PTEN partially by inhibiting Sp1, and activates PTEN and inactivates AKT | 25770423 |
| SACC-83 | Apoptosis Assay | 20 μM | 24 h | enhances radiation-induced inhibition of cell apoptosis | 25770423 |
| HeLa | Apoptosis Assay | 20 μM | 24 h | enhances radiation-induced inhibition of cell apoptosis | 25770423 |
| SACC-83 | Growth Inhibition Assay | 20 μM | 24 h | enhances radiation-induced inhibition of cell proliferation | 25770423 |
| HeLa | Growth Inhibition Assay | 20 μM | 24 h | enhances radiation-induced inhibition of cell proliferation | 25770423 |
| PANC-1 | Function Assay | 20/60/100 μM | 24 h | attenuats cell invasion and migration in a concentration-dependent manner | 25973062 |
| PANC-1 | Growth Inhibition Assay | 20/60/100 μM | 24/48/72 h | inhibits cell growth in both time and dose dependent manner | 25973062 |
| TAF | Function Assay | 10 µM | 48 h | increases EGFR mRNA and protein expression | 25987127 |
| TAF | Function Assay | 10 µM | 30-120 min | poorly affects dAkt phosphorylation consequent to EGF signaling | 25987127 |
| TAF | Function Assay | 10 µM | 7 d | affects TAFs adhesive properties | 25987127 |
| H357 | Growth Inhibition Assay | 7.5/10 μM | 48 h | inhibits cell growth combined with Sabutoclax | 26009874 |
| SGC-7901/DDP | Function Assay | 10 µM | 24 h | causes a marked decrease in the level of Bcl-2 protein | 26407653 |
| SGC-7901/DDP | Function Assay | 10 µM | 24 h | inhibits the expression of P-glycoprotein through blocking EP2, and inactivating PKA and CREB | 26407653 |
| SGC-7901/DDP | Apoptosis Assay | 10 µM | 24 h | induces apoptosis combined with with cisplatin | 26407653 |
| SGC-7901/DDP | Function Assay | 10 µM | 24 h | inhibits cyclooxygenase-2 and P-glycoprotein expression | 26407653 |
| HCC827 | Apoptosis Assay | 80 µM | 48 h | induces apoptosis | 26464643 |
| A549 | Apoptosis Assay | 80 µM | 48 h | induces apoptosis | 26464643 |
| HCC827 | Growth Inhibition Assay | 5-160 μM | 48 h | IC50=69.2 μM | 26464643 |
| A549 | Growth Inhibition Assay | 5-160 μM | 48 h | IC50=163.4 μM | 26464643 |
| CaES-17 | Apoptosis Assay | 20 μM | 48 h | reduces oxaliplatin-induced apoptosis | 26474693 |
| HKESC-2 | Apoptosis Assay | 20 μM | 48 h | reduces oxaliplatin-induced apoptosis | 26474693 |
| CaES-17 | Growth Inhibition Assay | 20 μM | 48 h | significantly increases the IC50 values of oxaliplatin | 26474693 |
| HKESC-2 | Growth Inhibition Assay | 20 μM | 48 h | significantly increases the IC50 values of oxaliplatin | 26474693 |
| H460 | Function Assay | 0.1-30 μM | 48 h | induces ICAM-1 expression on both protein and mRNA level | 26513172 |
| A549 | Function Assay | 0.1-30 μM | 48 h | induces ICAM-1 expression on both protein and mRNA level | 26513172 |
| PC-3 | Growth Inhibition Assay | 0-50 μM | 48 h | inhibits cell growth in a dose dependent manner | 24127882 |
| PC-3 | Cell Viability Assay | 0-100 μM | 72 h | decreases cell viability in a dose dependent manner | 24127882 |
| A549 | Function assay | 5 uM | 10 mins | Inhibition of mPGES1 in IL1-beta induced human A549 cells assessed as PGE2 production at 5 uM preincubated for 10 mins | 19884011 |
| PANC1 | Function assay | 25 to 50 M | 30 mins | Inhibition of IL-6-induced STAT3 phosphorylation in human PANC1 cells at 25 to 50 M pretreated 2 hrs prior to IL-6 challenge measured after 30 mins | 21678971 |
| HCA-7 | Function assay | 5 uM | 24 hrs | Inhibition of hyaluronan-induced CD44v6 in human HCA-7 cells transfected with Has2cDNA assessed as downregulation of 5-LOX protein expression at 5 uM after 24 hrs by Western blotting analysis | 24295787 |
| HCA-7 | Function assay | 5 uM | 24 hrs | Inhibition of hyaluronan-induced CD44v6 in human HCA-7 cells transfected with Has2cDNA assessed as downregulation of COX-2 protein expression at 5 uM after 24 hrs by Western blotting analysis | 24295787 |
| HCA-7 | Function assay | 5 uM | 24 hrs | Inhibition of hyaluronan-induced CD44v6 in human HCA-7 cells transfected with Has2cDNA assessed as downregulation of COX-1 protein expression at 5 uM after 24 hrs by Western blotting analysis | 24295787 |
| HeLa | Function assay | 100 uM | 24 hrs | Inhibition of mPGES-1 in human HeLa cells using PGH2 as substrate assessed as inhibition of IL-1beta/TNFalpha-stimulated PGE2 production at 100 uM after 24 hrs by LC-MS/MS analysis | 24183739 |
| HeLa | Function assay | 0.1 uM | 24 hrs | Inhibition of PGE2 secretion in human HeLa cells at 0.1 uM after 24 hrs by EIA monoclonal assay | 27349331 |
| RAW264.7 | Antiinflammatory assay | 20 uM | 2 hrs | Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS induced cox-2 expression at 20 uM preincubated for 2 hrs followed by LPS challenge measured after 24 hrs by Western blot method | 29100799 |
| RAW264.7 | Antiinflammatory assay | 20 uM | 2 hrs | Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS induced iNOS expression at 20 uM preincubated for 2 hrs followed by LPS challenge measured after 24 hrs by Western blot method | 29100799 |
| A549 | Function assay | 5 uM | Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation at 5 uM by cell-intact assay | 19053751 | |
| HT29 | Function assay | 10 uM | Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HT29 cells assessed as decrease in 5-LOX expression at 10 uM | 23517721 | |
| HT29 | Function assay | 10 uM | Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HT29 cells assessed as decrease in COX-2 expression at 10 uM | 23517721 | |
| 201T | Growth Inhibition Assay | 72 h | IC50=48.6 µM | 25057941 | |
| 273T | Growth Inhibition Assay | 72 h | IC50=80.5 µM | 25057941 | |
| SGC-7901/DDP | Growth Inhibition Assay | 24 h | IC50=35.45 μM | 26407653 | |
| SGC-7901 | Growth Inhibition Assay | 24 h | IC50=115.08 μM | 26407653 | |
| HCA-7 | Function assay | 72 hrs | Inhibition of IL-1beta-induced PGE2 production in human HCA-7 cells after 72 hrs by EIA, EC50 = 0.00115 μM. | 22516282 | |
| insect cells | Function assay | 1 min | Inhibition of human recombinant COX2 expressed in insect cells using arachidonic acid as substrate incubated for 1 min prior to substrate addition measured for 25 secs by TMPD-based chromogenic assay, IC50 = 0.042 μM. | 23010270 | |
| HNSCC 1483 | Function assay | 30 mins | Inhibition of COX-2 in human HNSCC 1483 cells using [14C] arachidonic acid as substrate preincubated for 30 mins before substrate addition measured after 30 mins, IC50 = 0.054 μM. | 22263894 | |
| J774 | Function assay | 15 mins | Inhibition of COX2 in LPS-stimulated mouse J774 cells assessed as inhibition of PGE2 production after 15 mins by radioimmunoassay, IC50 = 0.06 μM. | 18752957 | |
| J774 | Function assay | 24 hrs | Inhibition of COX-2-mediated PGE2 production in LPS-stimulated mouse J774 cells after 24 hrs by radioimmunoassay, IC50 = 0.061 μM. | 21992176 | |
| Sf21 | Function assay | 5 mins | Inhibition of recombinant N-terminal His6-tagged human COX-2 expressed in Baculovirus infected Sf21 cells using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 1 hr, IC50 = 0.26 μM. | 30293795 | |
| SF9 | Function assay | 15 mins | Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay, IC50 = 0.643 μM. | 29500130 | |
| HT-29 | Cytotoxicity assay | 48 hrs | Cytotoxicity against COX-2 positive human HT-29 cells transfected with CD44v6shRNA assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 0.7 μM. | 24295787 | |
| SF9 | Function assay | 15 mins | Inhibition of recombinant Leishmania donovani chagasi beta-carbonic anhydrase expressed in baculovirus infected insect Sf9 cells incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay, Ki = 0.705 μM. | 23977960 | |
| HCA-7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against COX-2 positive human HCA-7 cells transfected with CD44v6shRNA assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 0.75 μM. | 24295787 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay, IC50 = 0.76 μM. | 26346367 | |
| SF9 | Function assay | 15 mins | Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence ass, IC50 = 1.185 μM. | 29500130 | |
| RAW264.7 | Antiinflammatory assay | 18 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA, IC50 = 1.28 μM. | 24679441 | |
| APC10.1 | Cytotoxicity assay | 48 hrs | Cytotoxicity against COX-2 positive mouse APC10.1 cells transfected with CD44v6shRNA overexpressing HAS-2 assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 1.3 μM. | 24295787 | |
| RAW264.7 | Antiinflammatory assay | 30 mins | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 30 mins followed by LPS stimulation measured after 24 hrs by Griess assay, IC50 = 1.6 μM. | 26444098 | |
| RAW264.7 | Antiinflammatory assay | 18 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by griess reaction analysis, IC50 = 1.84 μM. | 24679441 | |
| HCA-7 | Cytotoxicity assay | 18 hrs | Cytotoxicity against human HCA-7 cells assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 2 μM. | 23517721 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay, IC50 = 2.15 μM. | 26346367 | |
| Escherichia coli Arctic cells | Function assay | 15 mins | Inhibition of recombinant Streptococcus mutans UA159 beta-carbonic anhydrase expressed in Escherichia coli Arctic cells preincubated for 15 mins by stopped flow CO2 hydrase assay, Ki = 2.425 μM. | 25913199 | |
| HT-29 | Cytotoxicity assay | 18 hrs | Cytotoxicity against human HT-29 cells assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 3 μM. | 23517721 | |
| J774 | Function assay | 15 mins | Inhibition of COX1 in arachidonic acid-stimulated mouse J774 cells assessed as inhibition of PGE2 production after 15 mins by radioimmunoassay, IC50 = 3.7 μM. | 18752957 | |
| J774 | Function assay | 15 mins | Inhibition of COX-1-mediated PGE2 production in arachidonic acid-stimulated mouse J774 cells incubated for 15 mins prior to arachidonic acid-challenge by radioimmunoassay, IC50 = 3.84 μM. | 21992176 | |
| J774 | Function assay | 15 mins | Inhibition of COX1 in mouse J774 cells using arachidonic acid as substrate assessed as inhibition of PGE2 production incubated for 15 mins prior to substrate addition measured after 30 mins by radioimmunoassay, IC50 = 3.84 μM. | 23680444 | |
| APC10.1 | Cytotoxicity assay | 18 hrs | Cytotoxicity against mouse APC10.1 cells assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 4.2 μM. | 23517721 | |
| B16F10 | Antiproliferative assay | 24 hrs | Antiproliferative activity against mouse B16F10 cells after 24 hrs by MTT assay, IC50 = 4.56 μM. | 25866240 | |
| SH-SY5Y | Antineurotoxicity assay | 72 hrs | Antineurotoxicity in human SH-SY5Y cells assessed as inhibition human THP1 cell supernatant-induced cytotoxicity compound pretreated 24 to 48 hrs to THP1 cells measured after 72 hrs of supernatant addition, IC50 = 5 μM. | 20138770 | |
| THP1 | Neuroprotective assay | 72 hrs | Neuroprotective activity against LPS and IFN-gamma-stimulated neurotoxin production in human THP1 cell assessed as inhibition of THP1 cell secretion-induced toxicity to human SH-SY5Y cells after 72 hrs by MTT assay, IC50 = 5 μM. | 20609589 | |
| MCF7 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 5.94 μM. | 25866240 | |
| APC10.1 | Function assay | 18 hrs | Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in mouse APC10.1 cells expressing Has2 assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 6 μM. | 23517721 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay, IC50 = 6.88 μM. | 26346367 | |
| HeLa | Antiproliferative assay | 24 hrs | Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay, IC50 = 7.35 μM. | 25866240 | |
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay, IC50 = 7.55 μM. | 26346367 | |
| HeLa | Antiproliferative assay | 24 hrs | Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay, IC50 = 7.79 μM. | 27349331 | |
| HepG2 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay, IC50 = 10.03 μM. | 27349331 | |
| B16F10 | Antiproliferative assay | 24 hrs | Antiproliferative activity against mouse B16F10 cells after 24 hrs by MTT assay, IC50 = 14.36 μM. | 27349331 | |
| A549 | Antitumor assay | 48 hrs | Antitumor activity against human A549 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50 = 15.6 μM. | 23353741 | |
| A549 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human A549 cells after 24 hrs by MTT assay, IC50 = 15.64 μM. | 27349331 | |
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, IC50 = 15.69 μM. | 30031652 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 16.08 μM. | 30031652 | |
| NCI60 | Growth inhibition assay | 48 hrs | Growth inhibition of human NCI60 cells after 48 hrs by sulforhodamine B assay, GI50 = 17.5 μM. | 20387815 | |
| HCA-7 | Function assay | 18 hrs | Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HCA-7 cells expressing Has2 assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 17.5 μM. | 23517721 | |
| HT-29 | Function assay | 18 hrs | Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HT-29 cells expressing Has2 assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 18.3 μM. | 23517721 | |
| B16F10 | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay, IC50 = 19.15 μM. | 30031652 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 26.78 μM. | 30031652 | |
| LNCAP | Cytotoxicity assay | 72 hrs | Cytotoxicity against human LNCAP cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 32.6 μM. | 28057407 | |
| BL21(DE3) | Function assay | 15 mins | Inhibition of GST-tagged Malassezia globosa ATCC 96807/CBS 7966 MG-CA expressed in Escherichia coli BL21(DE3) cells preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method, Ki = 34.8 μM. | 22424239 | |
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTS assay, IC50 = 40 μM. | 22780961 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT colorimetric assay, IC50 = 40.8 μM. | 22000948 | |
| MCF7 | Antitumor assay | 48 hrs | Antitumor activity against human MCF7 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50 = 40.8 μM. | 23353741 | |
| HCT116 | Anticancer assay | 72 hrs | Anticancer activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 43.3 μM. | 21678971 | |
| L1210 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse L1210 cells after 72 hrs by MTT assay, IC50 = 44 μM. | 20451397 | |
| PC3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against androgen-independent human PC3 cells after 72 hrs by MTT test, IC50 = 47 μM. | 15566290 | |
| PC3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50 = 48 μM. | 17937972 | |
| PC3 | Function assay | 2 hrs | Inhibition of PDK1-mediated Akt activation in human PC3 cells after 2 hrs by Western blotting analysis, IC50 = 48 μM. | 23735281 | |
| PC3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50 = 48.5 μM. | 20451397 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 49.66 μM. | 29191502 | |
| CHO | Function assay | In vitro inhibitory potency against human COX-2 in stably transfected chinese hamster ovary (CHO) cells, IC50 = 0.002 μM. | 10576684 | ||
| CHO | Function assay | Inhibition of PGE-2 production in CHO cells expressing human COX-2, IC50 = 0.002 μM. | 10576685 | ||
| CHO | Function assay | In vitro potency against human Prostaglandin G/H synthase 2 in transfected CHO cells, IC50 = 0.002 μM. | 10197970 | ||
| CHO | Function assay | Inhibitory of human Prostaglandin G/H synthase 2 expressed in CHO cells, IC50 = 0.002 μM. | 12643942 | ||
| synovial cells | Function assay | Inhibitory effect on production of cyclooxygenase-2 (COX-2) prostaglandin E2 (PGE2) in human IL1-beta stimulated synovial cells, IC50 = 0.0079 μM. | 10821716 | ||
| RAW264.7 | Function assay | Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production treated prior to LPS challenge by enzyme immunoassay, IC50 = 0.0087 μM. | 24656662 | ||
| HEK293 | Function assay | Inhibition of cloned Stylophora pistillata alpha-CA expressed in human HEK293 cells by stopped-flow CO2 assay, Ki = 0.0342 μM. | 19520577 | ||
| SF9 | Function assay | Inhibitory activity against human Prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus, IC50 = 0.036 μM. | 14698190 | ||
| SF9 | Function assay | In vitro inhibitory activity against human recombinant prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus, IC50 = 0.036 μM. | 15026050 | ||
| CHO | Function assay | Inhibition of COX2 expressed in CHO cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay, IC50 = 0.036 μM. | 15566290 | ||
| J774 | Function assay | Inhibition of COX2 in LPS-stimulated J774 cells assessed as inhibition of PGE2 levels by radioimmunoassay, IC50 = 0.06 μM. | 17915854 | ||
| J774 | Function assay | Inhibition of COX2 in mouse J774 cells assessed as inhibition of LPS-induced PGE2 production by radioimmunoassay, IC50 = 0.061 μM. | 23680444 | ||
| SF9 | Function assay | Inhibition of human COX2 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay, IC50 = 0.063 μM. | 19520573 | ||
| COS | Function assay | Inhibition of human cyclooxygenase-2 expressed in COS cells, IC50 = 0.068 μM. | 15454242 | ||
| COS | Function assay | Inhibition of human COX2 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay, IC50 = 0.068 μM. | 19520573 | ||
| 143982 | Function assay | In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells, IC50 = 0.079 μM. | 12877584 | ||
| J774 | Function assay | In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells, IC50 = 0.079 μM. | 15857149 | ||
| J774 | Function assay | Inhibition of COX2-dependent PGE2 production in LPS-stimulated mouse J774 cells by RIA, IC50 = 0.079 μM. | 19957931 | ||
| osteosarcoma cells | Function assay | Inhibition of Prostaglandin G/H synthase 2 in 143.98.2 from human osteosarcoma cells, IC50 = 0.08 μM. | 11462976 | ||
| SF9 | Function assay | Inhibition of human COX2 expressed in sf9 cells, IC50 = 0.08 μM. | 16252917 | ||
| RAW264.7 | Antiinflammatory assay | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production, IC50 = 0.1 μM. | 22000948 | ||
| RAW264.7 | Function assay | Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production, IC50 = 0.12 μM. | 23353741 | ||
| Sf21 | Function assay | Inhibition of recombinant human N-terminal His-tagged COX2 expressed in baculovirus infected Sf21 cells assessed as reduction in prostaglandin production by enzyme immunoassay, IC50 = 0.15 μM. | 29373271 | ||
| MC9 | Function assay | Inhibition of PGF2apha production in arachidonic acid-stimulated mouse MC9 cells, IC50 = 0.3 μM. | 18498150 | ||
| MC9 | Function assay | Inhibition of PGF2alpha production in mouse MC9 cells, IC50 = 0.4 μM. | 18498150 | ||
| 293E | Function assay | Inhibition of human microsomal PGES1 expressed in 293E cells by LC/MS/MS analysis, IC50 = 0.425 μM. | 26653180 | ||
| COS | Function assay | Inhibition of human cyclooxygenase-1 expressed in COS cells, IC50 = 1.689 μM. | 15454242 | ||
| COS | Function assay | Inhibition of human COX1 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 treated 1 hr before arachidonic acid challenge by enzyme immunoassay, IC50 = 1.689 μM. | 19520573 | ||
| J774 | Function assay | Inhibition of COX1 in mouse J774 cells assessed as arachidonic acid-induced PGE2 levels by radio immunoassay, IC50 = 3.7 μM. | 17915854 | ||
| HCA-7 | Cytotoxicity assay | Cytotoxicity against COX-2 positive human HCA-7 cells assessed as growth inhibition by CellTiter-96 AQueous assay, IC50 = 4.9 μM. | 24295787 | ||
| U-937 | Function assay | Inhibition of Prostaglandin G/H synthase 1 in U-937 cells from human histiocytic lymphoma, IC50 = 5.1 μM. | 11462976 | ||
| U-937 | Function assay | In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells, IC50 = 5.1 μM. | 12877584 | ||
| J774 | Function assay | In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells, IC50 = 5.1 μM. | 15857149 | ||
| J774 | Function assay | Inhibition of COX1-dependent PGE2 production in LPS-stimulated mouse J774 cells by RIA, IC50 = 5.1 μM. | 19957931 | ||
| HT-29 | Cytotoxicity assay | Cytotoxicity against COX-2 positive human HT-29 cells assessed as growth inhibition by CellTiter-96 AQueous assay, IC50 = 5.7 μM. | 24295787 | ||
| SW480 | Cytotoxicity assay | Cytotoxicity against COX-2 negative human SW480 cells assessed as growth inhibition by CellTiter-96 AQueous assay, IC50 = 6.9 μM. | 24295787 | ||
| APC10.1 | Cytotoxicity assay | Cytotoxicity against COX-2 positive mouse APC10.1 cells overexpressing HAS-2 assessed as growth inhibition by CellTiter-96 AQueous assay, IC50 = 13.4 μM. | 24295787 | ||
| CHO | Function assay | Inhibition of COX1 expressed in CHO cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay, IC50 = 13.5 μM. | 15566290 | ||
| platelet | Function assay | Inhibitory effect on production of cyclooxygenase-1 (COX-1) thromboxane B2 (TXB2) in human platelet cells, IC50 = 19 μM. | 10821716 | ||
| MDA231 | Antiproliferative assay | Antiproliferative activity against human MDA231 cells by MTT assay, IC50 = 22.79 μM. | 30216848 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells by MTT assay, IC50 = 29.54 μM. | 30216848 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells by MTT assay, IC50 = 31.28 μM. | 30216848 | ||
| HeLa | Antiproliferative assay | Antiproliferative activity against human HeLa cells by MTT assay, IC50 = 36.08 μM. | 30216848 | ||
| Caco2 | Antiproliferative assay | Antiproliferative activity against human Caco2 cells by MTT assay, IC50 = 42.74 μM. | 30216848 | ||
| HT-29 | Cytotoxicity assay | Cytotoxicity against human HT-29 cells by MTT assay, IC50 = 45.5 μM. | 20804197 | ||
| PC3 | Anticancer assay | Anticancer activity against human PC3 cells, GI50 = 47 μM. | 18262309 | ||
| A549 | Function assay | Inhibition of COX2-dependent PGE2 production in IL1B stimulated human A549 cells in presence of arachidonic acid | 18498150 | ||
| A549 | Function assay | Inhibition of COX2-dependent PGE2 production in IL1B stimulated human A549 cells | 18498150 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Celecoxib是一种选择性COX-2抑制剂，在Sf9细胞中IC50为40 nM。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在体外, Celecoxib有效选择性抑制COX-2，IC50为40 nM, 而作用于COX-1时，IC50为15 μM。[1]Celecoxib 作用于鼻咽癌 (NPC)细胞系，包括 HNE1和CNE1-LMP1，具有抗增殖效果，IC50分别为32.86 μM 和 61.31 μM。[4] |
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|---|---|---|---|---|
| 激酶实验 | 体外COX酶实验 | |||
| 细胞匀浆与COX-1或COX-2杆状病毒温育3天，通过测评PG合成能力，而测定昆虫细胞中COX蛋白表达。搅匀表达COX-1或COX-2的细胞，然后与花生四烯酸 (10 μM)混合。通过监测PG产量，而测定COX活性。在模拟感染的Sf9细胞中检测不出COX活性。Celecoxib与天然1% CHAPS 匀浆(2-10 μg 蛋白)预温育10分钟，然后加入花生四烯酸。温育10分钟后，通过ELISA检测形成的PGE2。 | ||||
| 细胞实验 | 细胞系 | HNE1和CNE1-LMP1 | ||
| 浓度 | 0 到75 μM | |||
| 孵育时间 | 48 小时 | |||
| 方法 | 使用MTT实验测定 Celecoxib 作用于 NPC细胞的抗增殖效果。细胞接种在96孔板上，粘附24小时。使用浓度不断增高的Celecoxib (0 到 75 μM) （溶于 DMSO， 终浓度 ≤0.1%)处理细胞，然后再温育48小时。 温育后，每孔加入 20 μL MTT 染料 (5 mg/mL) ，然后在37oC下温育4小时。移除上清液，晶体溶解在 DMSO 中，然后在490 nm处测定吸光值。使用 Probit回归模型及SPSS 15.0 软件计算IC50值和95%置信区间。每组实验至少重复进行三次。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | pAKT / AKT / PPARγ / PTEN COX-2 Fibronectin / Vimentin / N-cadherin / E-cadherin |
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24721996 | |
| Immunofluorescence | PPARγ / PTEN |
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24721996 | |
| Growth inhibition assay | Cell viability |
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28521485 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在体内, Celecoxib 具有有效的口服抗炎活性。Celecoxib 降低卡拉胶水肿检测中的急性炎症，也降低佐剂性关节炎模型中的慢性炎症，ED50分别为7.1 mg/kg和 0.37 mg/kg/day。此外, Celecoxib作用于Hargreaves 痛模型，也具有镇痛活性，ED50为34.5 mg/kg。此外, Celecoxib 按200 mg/kg剂量处理大鼠，不会产生急性GI毒性，每天按600 mg/kg剂量处理大鼠，持续10天以上，不会产生GI毒性。[1]13.5 Gy 局部胸部照射(LTI)142天(范围为 94-155 天)后，Celecoxib 作用于C3Hf/KamLaw 雌性小鼠模型，提高105天的平均寿命 (范围为79-145 天)。[5] |
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|---|---|---|
| 动物实验 | Animal Models | 溶于0.9%生理盐水的0.1 mL 1%卡拉胶溶液或溶于50 μL 矿物油的1 mg 乳酸分枝杆菌注射到雄性Sprague−Dawley大鼠右后腿足垫 |
| Dosages | ≤200 mg/kg | |
| Administration | 口服处理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01344200 | Recruiting | Pharmacokinetics of Celecoxib in Children |
Children''s Hospital of Eastern Ontario |
January 29 2024 | Phase 2 |
| NCT05648916 | Enrolling by invitation | Heterotopic Ossification |
McGill University Health Centre/Research Institute of the McGill University Health Centre |
August 2 2022 | -- |
| NCT05256823 | Active not recruiting | To Evaluate the Safety and Efficacy of Celecoxib Plus Nucleos(t)Ide Analogues in Nucleos(t)Ide-treated Patients With Chronic Hepatitis B |
Lai Wei|Beijing Tsinghua Chang Gung Hospital |
February 24 2022 | Phase 2 |
| NCT05324163 | Completed | KNEE OSTEOARTHRITIS |
Jiangsu XinChen-Techfields Pharma Co. LTD. |
September 29 2021 | Phase 3 |
| NCT04526197 | Completed | Wilson Disease |
Alexion Pharmaceuticals Inc. |
July 7 2020 | Phase 1 |
化学信息&溶解度
| 分子量 | 381.37 | 分子式 | C17H14F3N3O2S |
| CAS号 | 169590-42-5 | SDF | Download Celecoxib SDF |
| Smiles | CC1=CC=C(C=C1)C2=CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)C(F)(F)F | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 76 mg/mL ( (199.28 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 76 mg/mL (199.28 mM) Water : Insoluble |
摩尔浓度计算器 |
|
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:
I am doing an animal experiment with mice and planning to administrate S1261 via oral gavage. what are your recommendations for diluting the compound?
回答：
For oral administration, Celecoxib can be dissolved in vehicle one: "0.5% methyl cellulose and 0.025% Tween-20", or the vehicle 2 "2% DMSO/30% PEG 300/5% Tween 80/ ddH2O".
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