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Tofacitinib Citrate

Catalog No. T2398 CAS 540737-29-9

Synonyms: CP-690550 citrate, Tasocitinib citrate, Tofacitinib (CP-690550) Citrate

Tofacitinib Citrate (CP-690550 citrate) is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Tofacitinib Citrate, CAS 540737-29-9

Pack Size	Availability	Price/USD
5 mg	In stock	$ 32.00
10 mg	In stock	$ 50.00
50 mg	In stock	$ 64.00
100 mg	In stock	$ 93.00
200 mg	In stock	$ 129.00
500 mg	In stock	$ 219.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.75%

Purity: 99.47%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Tofacitinib Citrate (CP-690550 citrate) is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
Targets&IC50	JAK2:20 nM (cell free), JAK1:112 nM (cell free), JAK3:1 nM (cell free)
In vitro	Although Tofacitinib (CP-690,550) was highly potent for JAK3 inhibition (enzyme inhibitory potency of 1 nM), it was 20- to 100-fold less potent for JAK2 and JAK1, respectively. CP-690,550 inhibited IL-2-induced proliferation with 30-fold greater potency than its effects on GM-CSF-induced proliferation. CP-690,550 demonstrated potent inhibition in the mixed lymphocyte reaction using murine, monkey, or human cells. Consistent with its mechanism of action, these cellular activities correlated with the ability of CP-690,550 to block IL-2-induced phosphorylation of JAK3 and one of its key substrates, STAT5 [1]. CP-690,550 treatment of murine factor-dependent cell Patersen-erythropoietin receptor (FDCP-EpoR) cells harboring human wild-type or V617F JAK2 resulted in inhibition of cell proliferation with an IC50 of 2.1 microM and 0.25 microM, respectively. CP-690,550 treatment of ex-vivo-expanded erythroid progenitors from JAK2(V617F)-positive PV patients resulted in specific, antiproliferative (IC50: 0.2 microM) and pro-apoptotic activity [2]. The pharmacological inhibition of JAK3 by tofacitinib synergistically enhanced the antitumor effects of IMA in CML cells [3].
In vivo	CP-690,550 treatment significantly prolonged graft survival as compared to vehicle. Four of 12 animals dosed with CP-690,550 (two from each dose group) survived to study termination with normal renal function and mild rejection as determined by histopathology [1]. Monotherapy of mice with tofacitinib quells Ab responses to an immunotoxin derived from the bacterial protein Pseudomonas exotoxin A, as well as to the model Ag keyhole limpet hemocyanin. Thousand-fold reductions in IgG1 titers to both Ags were observed 21 d post immunization. Tofacitinib treatment led to reduced numbers of CD127+ pro-B cells [4].
Kinase Assay	The JAK1, JAK2, and JAK3 kinase assays utilize a protein expressed in baculovirus-infected SF9 cells (a fusion protein of GST and the catalytic domain of human JAK enzyme) purified by affinity chromatography on glutathione sepharose. The substrate for the reaction was polyglutamic acid-tyrosine [PGT (4:1)], coated onto Nunc Maxi Sorp plates at 100 μg/mL overnight at 37 °C. The plates were washed three times, and JAK enzyme was added to the wells, which contained 100 μL of kinase buffer (50 mM HEPES, pH 7.3, 125 mM NaCl, 24 mM MgCl2) + ATP + 1 mM sodium orthovanadate). After incubation at room temperature for 30 min, the plates were washed three times. The level of phosphorylated tyrosine in a given well was determined by standard ELISA assay utilizing an anti-phosphotyrosine antibody [5].
Cell Research	Apoptotic cells were detected by flow cytometry using recombinant human Annexin-V conjugated with allophycocyanin. Briefly, after exposure to CP-690,550 for different periods of time, cells were washed in Ca2+-free PBS and resuspended in 100 μL of binding buffer (10 mM HEPES pH 7.4; 0.15 M NaC1; 5 mM KCl; 1 mM MgCl2; 1.8 mM CaCl2) to which Annexin-V-APC had been previously added. Cells were incubated for 20 min in the dark at room temperature, washed and resuspended in 0.3 mL binding buffer. Cells were analyzed on a FACSCalibur flow cytometer equipped with the Cell Quest Pro software [2].
Animal Research	Mice received tofacitinib in PEG300 (100 mg/ml) or vehicle alone (PEG300) by osmotic pump infusion (Alzet Model 2004, 0.25 μl/hour, 28 days). Four days prior to immunization, mice were anesthetized and their dorsal surface was shaved. A one cm incision was made on the back to create a subcutaneous pocket and insert the pump. The incision site was closed with wound clips. Mice were injected weekly (i.p.) with SS1P recombinant immunotoxin (RIT; 5 μg/mouse) beginning on day 0; control mice received injections of saline alone. Every week before SS1P or vehicle immunization, ~50 μl of blood was drawn to obtain serum samples. Sera were stored at ?80°C until analyzed [4].

Synonyms	CP-690550 citrate, Tasocitinib citrate, Tofacitinib (CP-690550) Citrate
Molecular Weight	504.49
Formula	C22H28N6O8
CAS No.	540737-29-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50.5 mg/mL (100 mM)

References and Literature

1. Changelian PS, et al. Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. Science. 2003 Oct 31;302(5646):875-8. 2. Manshouri T, et al. The JAK kinase inhibitor CP-690,550 suppresses the growth of human polycythemia vera cells carrying the JAK2V617F mutation. Cancer Sci. 2008 Jun;99(6):1265-73. 3. Yagi K, et al. Pharmacological inhibition of JAK3 enhances the antitumor activity of imatinib in human chronic myeloid leukemia. Eur J Pharmacol. 2018 Apr 15;825:28-33. 4. Onda M, et al. Tofacitinib suppresses antibody responses to protein therapeutics in murine hosts. J Immunol. 2014 Jul 1;193(1):48-55. 5. Flanagan ME, et al. Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection. J Med Chem. 2010 Dec 23;53(24):8468-84.

Related compound libraries

This product is contained In the following compound libraries：

EMA Approved Drug Library Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Lung Cancer Compound Library Immunology/Inflammation Compound Library Anti-Pancreatic Cancer Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

Tofacitinib Citrate 540737-29-9 Angiogenesis Apoptosis Chromatin/Epigenetic JAK/STAT signaling Microbiology/Virology Stem Cells Antifungal Antibacterial JAK Influenza Virus inhibit CP-690550 Citrate CP-690550 citrate CP-690550 CP690550 Citrate CP690550 Janus kinase CP 690550 Tasocitinib citrate Fungal CP 690550 Citrate Tasocitinib Citrate Tofacitinib Tofacitinib (CP-690550) Citrate Inhibitor Tasocitinib Bacterial inhibitor

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