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Angiogenesis JAK Tofacitinib Citrate

Tofacitinib Citrate

Catalog No. T2398   CAS 540737-29-9
Synonyms: CP-690550 citrate, Tasocitinib citrate, Tofacitinib (CP-690550) Citrate
Purity 99.75% Datasheet MSDS

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

Tofacitinib Citrate, CAS 540737-29-9
Pack Size Availability Price/USD Quantity
10 mg In stock 50.00
50 mg In stock 72.00
100 mg In stock 104.00
200 mg In stock 144.00
500 mg In stock 244.00
1 mL * 10 mM (in DMSO) In stock 50.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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Description Tofacitinib citrate is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
Targets&IC50 JAK1 :ic50 112nM,   JAK2 :ic50 20nM,   JAK3 :ic50 1nM,   Lck :ic50 3.87μM,   ROCK2 :ic50 3.4μM,  
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 Enzyme assays: 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 is polyglutamic acid-tyrosine [PGT (4:1)], coated onto Nunc Maxi Sorp plates at 100 μg/mL overnight at 37 °C. The plates are washed three times, and JAK enzyme is 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). For Tofacitinib citrate, it is also added for kinase assay at different doses. After incubation at room temperature for 30 min, the plates are washed three times. The level of phosphorylated tyrosine in a given well is determined by standard ELISA assay utilizing an anti-phosphotyrosine antibody.
Cell Research
Determination of growth inhibition by Tofacitinib citrate is performed using identical culture conditions for both FDCP-EpoR JAK2WT and JAK2V617F cell lines. Briefly, 1 × 105 cells/mL are cultured in 96-well flat-bottom plates at 37 °C in a humidified 5% CO2 atmosphere using RPMI 1640 supplemented with 1.25% FCS, and 5% WEHI supernatant. Decreased FCS concentration is necessary to prevent binding between Tofacitinib citrate and serum proteins. Growth inhibition assays are terminated by addition of 20 μL CellTiter96 One Solution Reagent. Flat-bottom plates are incubated for an additional 3 hours for MTT assay. Absorbance is determined at 595 nm on a BioTek Synergy-HT microplate reader. Results are the average standard deviation of three independent determinations.(Only for Reference)
Cell lines: FDCP-EpoR JAK2WT and JAK2V617F cell lines
Animal Research
Animal Model: Mauritius-origin adult cynomolgus monkeys
Synonyms CP-690550 citrate, Tasocitinib citrate, Tofacitinib (CP-690550) Citrate
Purity 98.00%
Appearance solid
Molecular Weight 504.49
Formula C22H28N6O8
CAS No. 540737-29-9

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 50.5 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

0.5% methylcellulose: 30 mg/mL

Citations

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:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Stem cell Differentiation Compound Library Epigenetics Compound Library FDA-approved Drug Library Immunology/Inflammation Compound Library Kinase Inhibitor Library Angiogenesis related Compound Library JAK STAT Compound Library Cell cycle related Compound Library

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