Celecoxib

別名：SC 58635

製品コード：S1261 純度：99.92%

セレコキシブは、40nMのIC50による選択的なCOX-2阻害剤です。

CAS No. 169590-42-5

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
100mg	JPY 22000	国内在庫あり
1g	JPY 59500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（103）

製品安全説明書

現在のバッチを見る：純度： 99.92%

99.92

Celecoxib関連製品

関連ターゲット	COX-1 COX-2	もっと見る
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関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Neuronal Signaling Compound Library CNS-Penetrant Compound Library Anti-alzheimer Disease Compound Library	もっと見る

シグナル伝達経路

COXシグナル伝達経路

COX阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
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生物活性

製品説明

セレコキシブは、40nMのIC50による選択的なCOX-2阻害剤です。

Targets

COX-2 ^[1]
(Sf9 cells)

40 nM

In Vitro
In vitro	Celecoxib shows low sensitivity against COX-1 with IC50 of 15 μM. ^[1] Celecoxib shows an anti-proliferative effect on nasopharyngeal carcinoma (NPC) cell lines including HNE1 and CNE1-LMP1 with IC50 of 32.86 μM and 61.31 μM, respectively. ^[2]
Kinase Assay	COX enzyme assay in vitro
Kinase Assay	Expression of COX protein in insect cells is determined by assessing PG-synthetic capability in homogenates from cells incubated for 3 days with COX-1 or COX-2 baculovirus. Cells expressing COX-1 or COX-2 are homogenized and incubated with arachidonic acid (10 μM). COX activity is determined by monitoring PG production. No COX activity is detected in mock-infected Sf9 cells. Celecoxib are preincubated with crude 1% CHAPS homogenates (2-10 μg of protein) for 10 minutes before addition of arachidonic acid. PGE2 formed is detected by ELISA after 10 minute incubation.
細胞実験	細胞株	HNE1 and CNE1-LMP1
	濃度	0-75 μM
	反応時間	48 hours
	実験の流れ	The antiproliferative effect of Celecoxib on NPC cells is assessed using an MTT assay. Cells are seeded into 96-well plates and allowed to attach for 24 hours. The cells are then treated with increasing concentrations of Celecoxib (0 to 75 μM) dissolved in DMSO (final concentration ≤0.1%) and incubated for up to 48 hours. After the incubation, 20 μL of MTT dye (5 mg/mL) are added to each well and cells are incubated at 37 °C for 4 hours. After removing the supernatants, the crystals are dissolved in DMSO and the absorbance is measured at 490 nm. The half-maximal inhibitory concentration (IC50) values and the 95% confidence intervals are calculated using probit regression using SPSS 15.0 software. The experiment is performed in triplicate and repeated at least three times.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	pAKT / AKT / PPARγ / PTEN COX-2 Fibronectin / Vimentin / N-cadherin / E-cadherin		24721996
	Immunofluorescence	PPARγ / PTEN		24721996
	Growth inhibition assay	Cell viability		28521485

In Vivo
In Vivo	Celecoxib exhibits a potent, oral anti-inflammatory activity. Celecoxib reduces acute inflammation in the carrageenan edema assay and chronic inflammation in the adjuvant arthritis model with ED50 of 7.1 mg/kg and 0.37 mg/kg/day, respectively. In addition, Celecoxib also exhibits analgesic activity in the Hargreaves hyperalgesia model with ED50 of 34.5 mg/kg. Besides, Celecoxib produces no acute GI toxicity in rats at doses up to 200 mg/kg and no chronic GI toxicity in rats at doses up to 600 mg/kg/day over 10 days. ^[1] In a C3Hf/KamLaw female mouse model, Celecoxib increases median survival time of 105 days (range, 79-145 days) after 13.5 Gy local thoracic irradiation (LTI) alone to 142 days (range, 94-155 days). ^[3]
動物実験	動物モデル	A 0.1 mL aliquot of a 1% solution of carrageenan in 0.9% sterile saline or 1 mg of Mycobacterium butyricum in 50 μL of mineral oil is administered to the right hind foot pad of male Sprague−Dawley rats.
	投与量	≤200 mg/kg
	投与経路	Administered via p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考
[1] Penning TD, et al. J Med Chem, 1997, 40(9), 1347-1365. [2] Liu DB, et al. Acta Pharmacol Sin, 2012, 33(5), 682-690. [3] Hunter NR, et al. Int J Radiat Oncol Biol Phys, 2012, doi:10.1016/j.ijrobp.2012.04.025.

参考

化学情報

分子量	381.37	化学式	C₁₇H₁₄F₃N₃O₂S
CAS No.	169590-42-5	SDF	Download Celecoxib SDFをダウンロードする
Smiles	CC1=CC=C(C=C1)C2=CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)C(F)(F)F
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 76 mg/mL ( (199.28 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 76 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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よくある質問（FAQ）

質問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".

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):