Tofacitinib

別名：CP-690550, Tasocitinib

製品コード：S2789 純度：99.98%

Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1. Tofacitinib inhibits the expression of antiapoptotic BCL-A1 and BCL-XL in human plasmacytoid dendritic cells (PDC) and induced PDC apoptosis.

CAS No. 477600-75-2

サイズ	価格(税別)	在庫状況
5mg	JPY 22000	国内在庫あり
10mg	JPY 35500	国内在庫あり
50mg	JPY 71500	国内在庫あり
100mg	JPY 101500	国内在庫あり
1g	JPY 295500	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（172）

製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

Tofacitinib関連製品

関連ターゲット	JAK1 JAK2 JAK3 Tyk2	もっと見る
関連製品	AZD1480 WP1066 Momelotinib (CYT387) Filgotinib (GLPG0634) AT9283 Gandotinib (LY2784544) TG101209 Cerdulatinib (PRT062070) hydrochloride Pacritinib NVP-BSK805 2HCl WHI-P154 FLLL32 Decernotinib (VX-509) CEP-33779 AZ 960 Cerdulatinib (PRT062070) ZM 39923 HCl XL019 BMS-911543 Curcumol Solcitinib Oclacitinib maleate Pyridone 6 Creatine Ritlecitinib (PF-06651600) Deucravacitinib (BMS-986165) Itacitinib (INCB39110) Peficitinib BD750 WHI-P97 JANEX-1 Brevilin A 1,2,3,4,5,6-Hexabromocyclohexane Brepocitinib (PF-06700841) FM-381 SAR-20347 Selective JAK3 inhibitor 1	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Tyrosine Kinase Inhibitor Library JAK/STAT compound library	もっと見る

シグナル伝達経路

JAKシグナル伝達経路

JAK阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
CD4+ T	Growth Inhibition Assay	100/500 nM	48 h	inhibits anti-CD3-induced CD4+ T cell proliferation	21884580
CD4+ T	Function Assay	100 nM	24/48 h	abrogates CD3-induced phosphorylation of STATs	21884580
T cells	Function Assay	0.1/0.3/1 μM	24 h	disrupts γc-chain cytokine signaling	21383241
CD4+ T	Function Assay	20/100/500 nM	48 h	inhibits the levels of IL-4, IFN-γ, IL-17A and IL-22	21884580
NK-cells	Immunosuppressive assay	1 to 5 mg/kg	4 weeks	Immunosuppressive activity in naive cynomolgus monkey assessed as effect on CD3-CD16+ NK cells at 1 to 5 mg/kg, po for 4 weeks	14593182
T-cells	Function assay	5 to 500 nM	1 hr	Inhibition of IL2-induced Stat5 phosphorylation in human CD4+ T cells at 5 to 500 nM after 1 hr by Western blot	19053756
SUM149PT	Function assay	3 uM	16 hrs	Induction of PTPN6 in human SUM149PT cells assessed as inhibition of STAT3 phosphorylation at 3 uM after 16 hrs by Western blotting analysis in presence of pervanadate	24978112
Hs578T	Function assay	3 uM	16 hrs	Induction of PTPN6 in human Hs578T cells assessed as inhibition of STAT3 phosphorylation at 3 uM after 16 hrs by Western blotting analysis in presence of pervanadate	24978112
T-cells	Function assay	50 to 300 nM	1 hr	Inhibition of JAK1/JAK3 in human CD4 positive T cells assessed as inhibition of IL4-stimulated STAT6 phosphorylation at 50 to 300 nM preincubated for 1 hr followed by IL-4 stimulation measured after 30 mins by immunoblot analysis	29852068
T-cells	Function assay	50 to 300 nM	1 hr	Inhibition of JAK1/JAK3 in human CD4 positive T cells assessed as inhibition of IL2-stimulated STAT5 phosphorylation at Tyr-695 residue at 50 to 300 nM preincubated for 1 hr followed by IL-2 stimulation measured after 30 mins by immunoblot analysis	29852068
T-cells	Function assay	>300 nM	1 hr	Inhibition of JAK1/JAK2/TYK2 in human CD4 positive T cells assessed as inhibition of IL6-stimulated STAT3 phosphorylation at >300 nM preincubated for 1 hr followed by IL-6 stimulation measured after 30 mins by immunoblot analysis	29852068
TALL-1	Function assay	1 uM	3 hrs	Inhibition of JAK3 in human TALL-1 cells assessed as inhibition of IL-2 induced STAT5 phosphorylation at 1 uM preincubated for 3 hrs followed by IL-2 induction measured after 30 mins by immunoblotting	26258521
BA/F3	Function assay	300 nM	3 hrs	Inhibition of JAK3 (unknown origin) expressed in mouse BA/F3 cells assessed as reduction of STAT5 phosphorylation at 300 nM after 3 hrs by immunoblotting analysis	26258521
OCL-AML5	Function assay	1 uM	3 hrs	Inhibition of JAK2 in human OCL-AML5 cells assessed as inhibition of GM-CSF induced STAT5 phosphorylation at 1 uM preincubated for 3 hrs followed by GM-CSF induction measured after 30 mins by immunoblotting	26258521
BA/F3	Function assay	1 uM	3 hrs	Inhibition of JAK3 (unknown origin) expressed in mouse BA/F3 cells at 1 uM preincubated for 3 hrs followed by pulldown with streptavidin beads by immunoblotting analysis	26258521
Huh7	Function assay	10 uM	30 mins	Inhibition of Tyk2 in human Huh7 cells assessed as reduction of IFNalpha5-induced STAT3 phosphorylation at 10 uM pre-incubated for 30 mins before IFNalpha5 stimulation for 30 mins mins by immunoblotting	26231159
Huh7	Function assay	10 uM	30 mins	Inhibition of Tyk2 in human Huh7 cells assessed as reduction of basal level STAT3 phosphorylation at 10 uM after 30 mins by immunoblotting	26231159
Huh7	Function assay	1 uM	30 mins	Inhibition of Tyk2 in human Huh7 cells assessed as reduction of IFNalpha5-induced STAT3 phosphorylation at 1 uM pre-incubated for 30 mins before IFNalpha5 stimulation for 30 mins mins by immunoblotting	26231159
YT	Function assay	30 ng/ml		Inhibition of IL2-induced JAK3 phosphorylation in human YT cells at 30 ng/ml by immunoblotting analysis	14593182
YT	Function assay	30 ng/ml		Inhibition of IL2-induced STAT5A phosphorylation in human YT cells at 30 ng/ml by immunoblotting analysis	14593182
YT	Function assay	30 ng/ml		Inhibition of IL2-induced STAT5B phosphorylation in human YT cells at 30 ng/ml by immunoblotting analysis	14593182
Sf9	Function assay		30 mins	Inhibition of human GST-fused JAK3 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 30 mins by ELISA, Ki = 0.0004 μM.	23668484
Sf9	Function assay		90 mins	Inhibition of human recombinant N-terminal GST-tagged JAK3 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay, IC50 = 0.0006 μM.	22087750
Sf9	Function assay		30 mins	Inhibition of human GST-fused JAK1 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 30 mins by ELISA, Ki = 0.0007 μM.	23668484
Sf9	Function assay		30 mins	Inhibition of human GST-fused JAK2 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 30 mins by ELISA, Ki = 0.0007 μM.	23668484
Sf9	Function assay		90 mins	Inhibition of human recombinant N-terminal GST-tagged JAK1 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay, IC50 = 0.003 μM.	22087750
Sf9	Function assay		90 mins	Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay, IC50 = 0.004 μM.	22087750
SF21	Function assay		10 mins	Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis, IC50 = 0.004 μM.	23541670
T-cells	Function assay		72 hrs	Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting, IC50 = 0.011 μM.	14593182
Ba/F3	Function assay		60 mins	Inhibition of TEL-fused JAK1 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay, IC50 = 0.026 μM.	22087750
TF1	Function assay		20 mins	Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins in presence of whole blood, EC50 = 0.043 μM.	23659214
Sf9	Function assay		90 mins	Inhibition of human recombinant N-terminal GST-tagged TYK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay, IC50 = 0.052 μM.	22087750
TF1	Function assay		20 mins	Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins prior to IL6-induction measured after 30 to 45 mins, EC50 = 0.053 μM.	22698084
TF1	Function assay		20 mins	Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins, EC50 = 0.053 μM.	23659214
Ba/F3	Function assay		60 mins	Inhibition of TEL-fused JAK3 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay, IC50 = 0.054 μM.	22087750
TF1	Function assay		20 mins	Inhibition of JAK2 in human TF1 cells assessed as inhibition of EPO-induced STAT5 phosphorylation incubated for 20 mins prior to EPO-induction measured after 30 to 45 mins, EC50 = 0.093 μM.	22698084
TF1	Function assay		20 mins	Inhibition of JAK2 in human TF1 cells assessed as inhibition of EPO-induced STAT5 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins, EC50 = 0.093 μM.	23659214
TF1	Function assay		2 hrs	Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis, IC50 = 0.095 μM.	27130359
CTLL-2	Antiproliferative assay		72 hrs	Antiproliferative activity against IL-2-stimulated mouse CTLL-2 cells expressing JAK1/JAK3 after 72 hrs by alamar blue assay, IC50 = 0.132 μM.	19762238
DND/L12	Function assay		30 mins	Inhibition of JAK3 in human DND/L12 cells after 30 mins by luciferase assay in presence of human serum albumin, IC90 = 0.16 μM.	14593182
Ba/F3	Function assay		60 mins	Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay, IC50 = 0.265 μM.	22087750
HUO3	Function assay		4 days	Inhibition of human GM-CSF-induced proliferation in human HUO3 cells assessed as [3H]thymidine incorporation after 4 days by scintillation counting, IC50 = 0.324 μM.	14593182
HU03	Function assay		72 hrs	Inhibition of GM-CSF-induced human HU03 cells proliferation after 72 hrs by [3H]thymidine incorporation assay, IC50 = 0.324 μM.	21105711
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK3 kinase after 72 hrs by alamar blue assay, IC50 = 0.57 μM.	19762238
T-cells	Function assay		3 days	Inhibition of cell proliferation of IL2-activated and CD3 and CD28 antibody-stimulated mouse CD4-positive T cells after 3 days by XTT assay, IC50 = 0.63 μM.	30460842
NK92	Function assay		20 mins	Inhibition of TYK2 in human NK92 cells assessed as inhibition of IL12-induced STAT4 phosphorylation incubated for 20 mins followed by IL12 challenge for 45 mins, EC50 = 0.71 μM.	23659214
Ba/F3	Function assay		60 mins	Inhibition of TEL-fused TYK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay, IC50 = 1.2 μM.	22087750
T-cells	Function assay		72 hrs	Inhibition of JAK3 in rat splenocytic T cells assessed as reduction in IL-2-induced cell proliferation after 72 hrs by MTS assay, IC50 = 1.2 μM.	30139575
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK2 kinase after 72 hrs by alamar blue assay, IC50 = 1.574 μM.	19762238
HEL	Function assay		1 hr	Inhibition of JAK2 V617F mutant in human HEL cells after 1 hr, IC50 = 4.724 μM.	27771180
Jurkat	Function assay		24 hrs	Inhibition of anti-CD3/anti-CD28-induced IL2 production in human Jurkat cells after 24 hrs by scintillation counting, IC50 = 7.84 μM.	14593182
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay	26258521
Sf9	Function assay			Inhibition of human recombinant GST-tagged JH1 domain (785 to1125) of JAK3 expressed in insect Sf9 cells by ELISA, IC50 = 0.001 μM.	14593182
Sf9	Function assay			Inhibition of GST-tagged human JAK3 catalytic domain expressed in Sf9 cells by ELISA, IC50 = 0.001 μM.	21105711
Sf9	Function assay			Inhibition of GST-tagged human JAK3 catalytic domain expressed in Sf9 cells by ELISA, IC50 = 0.0033 μM.	21105711
insect cells	Function assay			Inhibition of GST-tagged Jak1 expressed in insect cells using 70 uM ATP, IC50 = 0.0061 μM.	21155605
insect cells	Function assay			Inhibition of GST-tagged Jak3 expressed in insect cells using 18 uM ATP, IC50 = 0.008 μM.	21155605
insect cells	Function assay			Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATP, IC50 = 0.012 μM.	21155605
MO7	Function assay			Inhibition of Jak3-mediated IL15-induced Stat5 phosphorylation in human MO7 cells by cell-based assay, IC50 = 0.024 μM.	21155605
T-cells	Function assay			Inhibition of JAK3/1 in human T cells expressing CD3 assessed as inhibition of IL2-stimulated STAT5a phosphorylation, IC50 = 0.028 μM.	23540648
PBMC	Function assay			Inhibition IL-7-indcued STAT5 phosphorylation in human PBMC cells by flow cytometry, IC50 = 0.039 μM.	26927423
TF1	Function assay			Inhibition of JAK1 in human TF1 cells assessed as suppression of IL6-stimulated STAT3 phosphorylation by AlphaScreen assay, INH = 0.045 μM.	26372653
CTLL	Function assay			Inhibition of Jak3-mediated IL2-induced Stat5 phosphorylation in mouse CTLL cells by cell-based assay, IC50 = 0.048 μM.	21155605
TF1	Function assay			Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL2-induced STAT3 phosphorylation, EC50 = 0.053 μM.	22591402
T-cells	Function assay			Inhibition of allogenic cells-stimulated proliferation in monkey T cells by mixed lymphocyte reaction method, IC50 = 0.057 μM.	14593182
CD34+	Function assay			Inhibition of JAK2 in human CD34+ cells assessed as inhibition of EPO-mediated cell proliferation, IC50 = 0.071 μM.	26927423
TF1	Function assay			Inhibition of IL4-induced proliferation of TF1 cells, IC50 = 0.08 μM.	16934457
T-cells	Function assay			Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method, IC50 = 0.087 μM.	14593182
PBMC	Function assay			Inhibition of JAK1 in human PBMC cells assessed as inhibition of IL-6-induced MCP1 secretion, IC50 = 0.095 μM.	26927423
TF1	Function assay			Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay, IC50 = 0.107 μM.	29156136
Sf9	Function assay			Inhibition of GST-tagged human JAK1 catalytic domain expressed in Sf9 cells by ELISA, IC50 = 0.11 μM.	21105711
T-cells	Function assay			Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method, IC50 = 0.115 μM.	14593182
ME180	Function assay			Inhibition of JAK1 in IL6-stimulated human ME180 cells expressing stably integrated beta-lactamase reporter gene under control of sis-inducible element by fluorescence assay, IC50 = 0.124 μM.	29156136
HT2	Function assay			Inhibition of JAK3 in mouse HT2 cells assessed as suppression of cell growth, IC50 = 0.156 μM.	27771180
T-cells	Function assay			Inhibition of JAK2/1 in human T cells expressing CD3 assessed as inhibition of IFNgamma-stimulated STAT1 phosphorylation, IC50 = 0.17 μM.	23540648
insect	Function assay			Inhibition of GST-tagged Tyk2 expressed in insect cells using 35 uM ATP, IC50 = 0.176 μM.	21155605
TF1	Function assay			Inhibition of JAK2 in human TF1 cells assessed as suppression of cell growth, IC50 = 0.2751 μM.	27771180
CD34+	Function assay			Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis, IC50 = 0.302 μM.	24417533
TF1	Function assay			Inhibition of IL3-induced proliferation of TF1 cells, IC50 = 0.8 μM.	16934457
UT7	Function assay			Inhibition of JAK2 in human UT7 cells assessed as suppression of EPO-stimulated STAT5 phosphorylation by AlphaScreen assay, INH = 1.12 μM.	26372653
SZ4	Function assay			Inhibition of JAK3 in human SZ4 cells assessed as reduction in IL2-stimulated STAT5 phosphorylation preincubated for 1 hr followed by IL2 stimulation and measured after 15 mins by MSD assay, IC50 = 1.21 μM.	30460842
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生物活性

製品説明

Targets

JAK3 ^[1] (Cell-free assay)	JAK2 ^[1] (Cell-free assay)	JAK1 ^[1] (Cell-free assay)
1 nM	20 nM	112 nM

In Vitro
In vitro	CP-690550 is a specific, orally inhibitor of JAK3, it is 20- to 100-fold less potent for JAK2 and JAK1 with IC50 of 20 nM and 112 nM, respectively. CP-690550 doesn't have potent activity against 30 other kinases (all median IC50 > 3000 nM). CP-690,550 inhibits IL-2–induced proliferation with 30-fold greater potency than its effects on GM-CSF–induced proliferation. ^[1] CP-690550 effectively inhibits a murine mixed lymphocyte reaction (MLR) (IC50 = 91 nM). ^[2] CP-690550 potently inhibits IL-4 induced upregulation of CD23 (IC50=57 nM) and class II major histocompatibility complex (MHCII) expression (IC50=71 nM) on murine B cells. ^[3] A recent research indicates low dose of CP-690550 accelerates the onset of experimental autoimmune encephalomyelitis by potentiating Th17 differentiation. ^[4]
Kinase Assay	JAK3 Kinase Assay
Kinase Assay	A fragment encoding the catalytic domain of human JAK3 (785aa to 1125aa, JH1 catalytic domain) is amplified by PCR from the full length cDNA and cloned into the EcoRI site of the baculovirus transfer vector pVL1393. Recombinant baculovirus is used to infect Sf9 (Spodoptera frugipedra) cells and recombinant GSTJAK3 fusion protein is isolated on glutathione sepharose. The fusion protein is eluted with reduced glutathione and stored in buffer containing 50 mM Tris, pH 7.5, 10 mM DTT and 10% glycerol. JAK3 kinase activity is measured by ELISA as follows: Plates are coated overnight with a random L-glutamic acid and tyrosine co-polymer (4:1) (100 ug/mL). The plates are washed and recombinant JAK3 JH1:GST (100 ng/well) with or without inhibitors is incubated at room temperature for 30 minutes, after which HRP-conjugated PY20 anti-phosphotyrosine antibody (ICN) is added and developed by TMB (3,3',5,5'-tetramethylbenzidine). Other kinases (Table 1) are produced in E. coli or in insect cells, depending upon what is found to be optimal for the given kinase. The catalytic activity of tyrosine kinases is easured using the aftorementioned ELISA, whereas serine/threonine kinases are assayed using radioactive enzyme assays.
細胞実験	細胞株	Human T blasts cell
	濃度	0-4000 nM
	反応時間	4 days
	実験の流れ	To measure IL-2-dependent proliferation, isolated lymphocytes are resuspended to a cell density of 1-2 × 10⁶/mL in complete RPMI medium (RPMI 1640 containing 10% (w/v) fetal calf serum (FCS), 1%(w/v) penicillin and treptomycin).Phytohemagluttinin (PHA) is added to a final concentration of 10mg/mL, and the culture incubated for 3 days at 37 °C in a humidified 5% (v/v) CO₂ incubator to upregulate IL-2R and JAK3 expression. IL-2 (200U/mL), with or without CP-690,550 is then added and the cells are incubated for 72 hours at 37 °C in a humidified 5% (v/v) CO₂ incubator, after which 50 mL of ³H-thymidine (5mCi/mL) is added. The plates are incubated for an additional 18 hours, harvested with a 96-well harvester, and counted on a scintillation counter. HUO3 cells are maintained in culture with granulocyte-macrophage colony stimulating factor and human foreskin fibroblasts are maintained in culture with 10% fetal calf serum. CP-690550 is added to freshly plated cells and cultured for 4 days. 3Hthymidine is added during the last 18 hours of the culture period.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	JAK3 / STAT5 / p-STAT5 LMP1 / EBNA1 / BZLF1 JAK3 / p-JAK3 / STAT3		27732937
	Growth inhibition assay	Cell number		27732937

In Vivo
In Vivo	In a murine model of heterotopic heart transplantation (DBA2 donor heart into C57/BL6 host), CP-690550 results in a dose-dependent increase in survival of transplanted hearts.The EC50 (drug concentration in blood at which 50% of mice will maintain their graft for >28 days) to be ~60 ng/mL.CP-690550 prevents rejection of allogeneic kidneys in nonhuman primate (NHPs, macaca fascicularis) (MST of 62 and 83 days for the 50 to 100 ng/ml groups and 200 to 400 ng/ml groups, respectively). ^[1] Mice chronically dosed with CP-690550 (1.5-15 mg/kg/day) demonstrates dose and time-dependent alterations in lymphocyte subsets when examined by flow cytometry. The most dramatic change observed is a 96% reduction in splenic NK1.1+TCRb-cell numbers following 21 days of treatment. Delayed-type hypersensitivity (DTH) responses in sensitized mice are reduced in a dose-dependent manner following treatment with CP-690550 (1.87–30 mg/kg, s.c.). Extended survival of neonatal Balb/c hearts implanted into the ear pinna of MHC mismatched C3H/HEN mice is observed with CP-690550 monotherapy (10–30 mg/kg/day), but improved upon combination with cyclosporin (10 mg/kg/day). ^[2]
動物実験	動物モデル	DBA/2 and C57/BL6 mice
	投与量	0-136 ng/mL
	投与経路	Administered via osmotic minipump infusion

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06202560	Enrolling by invitation	Frontal Fibrosing Alopecia\|Lichen Planopilaris	Institute of Dermatology Thailand	November 29 2023	Not Applicable
NCT05487703	Completed	Arthritis Rheumatoid	Pfizer	November 14 2022	--
NCT05082428	Completed	Ulcerative Colitis	Pfizer	May 30 2022	--
NCT05728008	Completed	Ulcerative Colitis	IRCCS San Raffaele	April 5 2022	--
NCT04768504	Recruiting	Immune-Mediated Colitis	Khashayar Esfahani\|Sir Mortimer B. Davis - Jewish General Hospital	March 22 2022	Phase 2

参考
[1] Changelian PS, et al, Science, 2003, 302(5646), 875-878. [2] Kdlacz E, et al, Am J Transplant, 2004, 4(1), 51-57. [3] Kudlacz E, et al, Eur J harmacol, 2008, 582(1-2), 154-161. [4] Yoshida H, et al, Biochem Biophys Res Commun, 2012, 418(2), 234-240. [5] Borie DC, et al, Transplantation, 2005, 80(12), 1756-1764. [6] Kudlacz E, et al. Am J Transplant, 2004, 4(1), 51-57. + 展開

参考

+ 展開

化学情報

分子量	312.37	化学式	C₁₆H₂₀N₆O
CAS No.	477600-75-2	SDF	Download Tofacitinib SDFをダウンロードする
Smiles	CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N
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ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 62 mg/mL ( (198.48 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。)

Water : Insoluble

Ethanol : 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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* 大学・企業名 大学・企業名を記入してください

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よくある質問（FAQ）

質問1:
I was just wondering what the main differences between S2789 and S5001?

回答
S2789(Tofacitinib (CP-690550)) is the base form of S5001 (Tofacitinib (CP-690550) Citrate). The biological activity of these two compounds are same. The S5001 (Tofacitinib (CP-690550) Citrate) is more suitable for oral administration.

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):