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ChemicalBook >> CAS DataBase List >>Tofacitinib citrate

Tofacitinib citrate

CAS No.
540737-29-9
Chemical Name:
Tofacitinib citrate
Synonyms
Xeljanz;Tofacitnib Citrate;Tofacitinib (CP-690550) Citrate;Tofacitinib-d3 Citrate;(3R,4R)-1-(Cyanoacetyl)-4-methyl-N-methyl-N-1H-pyrrolo[2,3-d]pyrimidin-4-yl-3-piperidinamine 2-hydroxy-1,2,3-propanetricarboxylate;(3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-beta-oxo-1-piperidinepropanenitrile 2-Hydroxy-1,2,3-propanetricarboxylate;CS-656;CP 690550-10;CP 690500-10;Tofacitinib API
CBNumber:
CB92460269
Molecular Formula:
C16H20N6O.C6H8O7
Molecular Weight:
504.497
MDL Number:
MFCD11616529
MOL File:
540737-29-9.mol
MSDS File:
SDS
Last updated:2024-11-19 23:02:33

Tofacitinib citrate Properties

Melting point 201 °C (decomp)
storage temp. room temp
solubility DMSO: soluble5mg/mL (clear solution; warmed)
form powder
color white to beige
InChIKey SYIKUFDOYJFGBQ-YLAFAASESA-N
SMILES C1[C@@H](C)[C@@H](N(C2C3=C(NC=C3)N=CN=2)C)CN(C(CC#N)=O)C1.C(C(=O)O)C(C(=O)O)(O)CC(O)=O |&1:1,3,r|
FDA UNII O1FF4DIV0D

Pharmacokinetic data

Protein binding 40%
Excreted unchanged in urine 30%
Volume of distribution 87 Litres
Biological half-life 3 / 3.8

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H315-H319
Precautionary statements  P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313
WGK Germany  3
HS Code  29335990
NFPA 704
0
2 0

Tofacitinib citrate price More Price(39)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich PZ0017 Tofacitinib citrate ≥98% (HPLC) 540737-29-9 5mg $127 2024-03-01 Buy
Sigma-Aldrich PZ0017 Tofacitinib citrate ≥98% (HPLC) 540737-29-9 25mg $505 2024-03-01 Buy
Cayman Chemical 11598 CP 690,550 ≥98% 540737-29-9 5mg $68 2024-03-01 Buy
Cayman Chemical 11598 CP 690,550 ≥98% 540737-29-9 10mg $130 2024-03-01 Buy
Cayman Chemical 25046 Tofacitinib-d3 (citrate) ≥99% deuterated forms (d1-d3) 540737-29-9 1mg $668 2024-03-01 Buy
Product number Packaging Price Buy
PZ0017 5mg $127 Buy
PZ0017 25mg $505 Buy
11598 5mg $68 Buy
11598 10mg $130 Buy
25046 1mg $668 Buy

Tofacitinib citrate Chemical Properties,Uses,Production

Description

Tofacitinib citrate, also known as CP-690550 citrate, is a king of drugs developed by the US pharmaceutical company Pfizer for treating rheumatoid arthritis, trade name Xeljanz, for the treatment of methotrexate inadequate response or intolerance to severe active rheumatoid arthritis (RA) in adult patients. This product is a Janus kinase inhibitor, administered twice daily.
November 6, 2012, the US Food and Drug Administration (FDA) and Pfizer jointly announced Tofacitinib citrate is approved for the treatment of methotrexate inadequate response or intolerance to severe active rheumatoid joints arthritis (RA) in adult patients.
Xeljanz can be used as monotherapy or in combination with methotrexate or other non-biological disease-modifying antirheumatic drugs (the DMARD) in combination. This medicine should not be in combination with biological DMARD or strong immunosuppressants (such as cyclosporine and azathioprine). Xeljanz is approved by the daily dose of 2 times, each time 5mg.
Seven clinical trials evaluated the safety and efficacy of Tofacitinib citrate in moderate to severe active RA in adult patients. In all tests, compared with patients receiving placebo, patients receiving Xeljanz treatment showed significant improvement in clinical response and physical function.
In Clinical trials, the most common adverse events were upper respiratory tract infection, headache, diarrhea, nasal congestion, sore throat, and nasopharyngitis.
Using Xeljanz was associated with an increased risk of serious infections, including opportunistic infections, tuberculosis, cancer and lymphoma. Xeljanz product label attaches boxed warning on these security risks. Xeljanz treatment is also associated with reducing blood cell counts and increasing cholesterol and liver enzyme values.
In order to study Xeljanz long-term impact on heart disease, cancer and severe infections, FDA requires for a post-marketing study, which will evaluate two doses of Xeljanz (Tofacitinib citrate) therapy, and accept a integration of another group of patients approved by the treatment as a control.

Uses

Tofacitinib citrate has been used:
as a ligand for human serum albumin in fluorescence quenching, dynamic light scattering (DLS) measurements, differential scanning calorimetry and molecular docking studies
as a medium supplement for full depth articular cartilage (FDC) explants to monitor cytokine-induced proteoglycan loss
as a Janus kinase inhibitor in MCF7 breast cancer cells

Definition

ChEBI: Tofacitinib citrate is a citrate salt obtained by combining equimolar amounts of tofacitinib and citric acid. Used to treat moderately to severely active Rheumatoid Arthritis. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor and an antirheumatic drug. It contains a tofacitinib.

General Description

Tofacitinib is a synthetic molecule corresponding to a molecular weight of 312.4 Da and is permeable by transcellular diffusion.

Biological Activity

tofacitinib citrate, also known as cp-690550 citrate, is a potent inhibitor of janus kinase 3 (jak3), a hematopoetic cell-restricted tyrosine kinase involved in signal transduction regulating lymphocyte survival, proliferation, differentiation, and apoptosis. the inhibition is jak3 specific with a selectivity 1000-fold more than other non-jak family kinases. besides inhibiting jaks (ic50 = 1 nm), tofacitinib citrate also inhibits janus kinase 2 (jak2) and janus kinase 1 (jak1) with 20- and 100-fold less in potency respectively. however, in a recent study, the binding affinities (ki) of tofacitinib citrate towards jak1, jak2, and jak3 were reported to be 1.6 nm, 21.7 nm, and 6.5 nm respectively.lalitha vijayakrishnan, r. venkataramanan and palak gulati. treating inflammation with the janus kinase inhibitor cp-690,550. trends in pharmacological sciences 2011: 32 (1); 25-34

Biochem/physiol Actions

Tofacitinib is a potent inhibitor of Janus kinase 3 (JAK3) with some JAK-1 inhibitory activity as well. It blocks downstream STAT signaling resulting in potent inhibition of inflammatory cytokines with resultant immunosuppressive and anti-inflammatory activity. Tofacitinib is being investigated for for several autoimmune disorders including, rheumatoid arthritis, psoriasis and dry eye.

Clinical Use

Potent, selective inhibitor of the Janus kinase family:
Treatment of moderate to severe active rheumatoid arthritis

Side effects

The most common side effects of Tofacitinib citrate are upper respiratory tract infection, headache, diarrhoea and nasopharyngitis. Other side effects that may occur are increased risk of infections (tuberculosis, hepatitis B, hepatitis C, herpes zoster), higher cholesterol levels, heart disease, stroke and blood clots. Very rare side effects are perforation of the colon, lymphoma and other malignancies.

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. CP-690550 effectively inhibits a murine mixed lymphocyte reaction (MLR) (IC50 = 91 nM). 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. A recent research indicates low dose of CP-690550 accelerates the onset of experimental autoimmune encephalomyelitis by potentiating Th17 differentiation.

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). Mice chronically dosed with CP-690550 (1.5-15 mg/kg/day) demonstrate 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.).

target

JAK3

Drug interactions

Potentially hazardous interactions with other drugs
Antibacterials: concentration of tofacitinib reduced by rifampicin - avoid.
Antifungals: concentration of tofacitinib increased by fluconazole and ketoconazole - adjust tofacitinib dose.
Antipsychotics: increased risk of agranulocytosis with clozapine - avoid.
Ciclosporin: concentration of tofacitinib reduced - avoid.
Tacrolimus: concentration of tofacitinib reduced - avoid.
Vaccines: risk of generalised infections with live vaccines - avoid.ccccccc

Metabolism

70% metabolised in the liver by CYP3A4 (major) and CYP2C19 (minor). The 8 metabolites produced are inactive.

References

1. The mechanism of action of tofacitinib - an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis. PMID: 26966791
2. Binding of Janus kinase inhibitor tofacitinib with human serum albumin: multi-technique approach DOI:10.1080/07391102.2015.1104522
3. Tofacitinib and TPCA-1 exert chondroprotective effects on extracellular matrix turnover in bovine articular cartilage ex vivo. DOI:10.1016/j.bcp.2018.07.034
4. Phosphoproteome profiling reveals critical role of JAK-STAT signaling in maintaining chemoresistance in breast cancer DOI:10.18632/oncotarget.21801
5. Lalitha Vijayakrishnan, R. Venkataramanan and Palak Gulati. Treating inflammation with the janus kinase inhibitor CP-690,550. Trends in Pharmacological Sciences 2011: 32 (1); 25-34 DOI:10.1016/j.tips.2010.10.004
6. http://www.medicinenet.com/tofacitinib_citrate_xeljanz/article.htm

Tofacitinib citrate Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Tofacitinib citrate manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Tofacitinib Citrate pictures 2024-12-20 Tofacitinib Citrate
540737-29-9
 US $0.00 / Kg/Bag 2Kg/Bag 99% up 20tons Sinoway Industrial co., ltd.
Tofacitinib citrate pictures 2024-12-13 Tofacitinib citrate
540737-29-9
 US $0.00-0.00 / g 1g 99%min 1000G WUHAN FORTUNA CHEMICAL CO., LTD
Tofacitinib Citrate pictures 2024-11-19 Tofacitinib Citrate
540737-29-9
 US $32.00-64.00 / mg 99.75% 10g TargetMol Chemicals Inc.

Tofacitinib citrate Spectrum

1-PIPERIDINEPROPANENITRILE, 4-METHYL-3-(METHYL-7H-PYRROLO[2,3-D]PYRIMIDIN-4-YLAMINO)-BETA-OXO-, (3R,4R)-, 2-HYDROXY-1,2,3-PROPANETRICARBOXYLATE (1:1) CP-690550 (Tofacitinib citrate) CP 690500-10 CP 690550-10 1-Piperidinepropanenitrile, 4-methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-beta-oxo-, (3R,4R)-, citrate 1-PIPERIDINEPROPANENITRILE, 4-METHYL-3-(METHYL-7H-PYRROLO[2,3-D]PYRIMIDIN-4-YLAMINO)-BETA-OXO-, (3R,4R)-, 2-HYDROXY-1,2,3-PROPANETRICARBOXYLATE Tofacitinib citrate, >=98% 1-Piperidinepropanenitrile, 4-Methyl-3-(Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-ylaMino)-β-oxo-, (3R,4R)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) Tofacitinib citrate (CP-690550) Tofacitinib citrate Tasocitinib citrate Tasocitinib citric acid s... 3-PiperidinaMine, 1-(cyanoacetyl)-4-Methyl-N-Methyl-N-1H-pyrrolo[2,3-d]pyriMidin-4-yl-, (3R,4R)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) 3-{(3R,4R)-4-Methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl}-3-oxopropanenitrile 2-hydroxy-1,2,3-propanetricarboxylate (1:1) Tofacitinib, Citrate Salt, >99% 3-{(3R,4R )-4-Methyl-3-[methyl(7H –pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl}-3-oxopropanenitrile monocitrate Tasocitinib citric acid salt 3-((3R,4R)-4-Methyl-3-(Methyl(7H-pyrrolo[2,3-d]pyriMidin-4-yl)aMino)piperidin-1-yl)-3-oxopropanenitrile citrate CP-690550 citrate Tofacitinib Citratet 3-{4-Methyl-3-[Methyl-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)-aMino]-piperidin-1-yl}-3-oxo-propionitrile Tofacitinib API Tofacitinib citric acid salt (3r,4r)-4-Methyl-3-(Methyl-7h-pyrrolo(2,3-d)pyriMidin-4-ylaMino)-beta-oxo-1 Tofacititinib cirate CP-690550 Citrate (Tofacitinib Citrate) Tofacitinib (Tasocitinib, CP-690550) (3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-beta-oxo-1-piperidinepropanenitrile 2-Hydroxy-1,2,3-propanetricarboxylate Tofacitinib citrate(CP690550) Tofacitinib citrate (3R,4R)-1-(Cyanoacetyl)-4-methyl-N-methyl-N-1H-pyrrolo[2,3-d]pyrimidin-4-yl-3-piperidinamine 2-hydroxy-1,2,3-propanetricarboxylate (3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-bet (3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-1-piperidinepropanenitrile citrate salt 3-[(3R,4R)-4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile citrate salt Tasocitinib citrate salt Xeljanz(tofacitinib) Citrate Tropsch iMatinib 1-Piperidinepropanenitrile,4-Methyl-3-(Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-ylaMino)-β-oxo-,(3R,4R)-,2-hydroxy-1,2,3-propanetricarboxylate 3-[(3R,4R)-4-Methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-1-piperidyl]-3-oxopropanenitrile 2-Hydroxypropane-1,2,3-tricarboxylate Tofacitinib citrate - CP 690550-10 Tofacitinib-13C-d3 Citrate CS-656 Tofacitinib citrate (CP-690553 citrate) ofacitinibcitrate 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile, citrate (1:1) Tofacitinib citrate ISO 9001：2015 REACH CP-690550 Citrate (Tofacitinib Citrate) DISCONTINUED tofacitinib citratoTofacitinib citrate Tofacitinib Citrate (API) (3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-1-piperidinepropanenitrile 1-Piperidinepropanenitrile, 4-methyl-3-(methyl-7H-pyrrolo[2,... tofacitinib citrate1004 tofacitinib citrate1005 3-((3R,4R)-4-Methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile 2-hydroxypropane-1,2,3-tricarboxylate (Tofacitinib Impurity) 1-Piperidinepropanenitrile, 4-methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-, (3R,4R)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) Tofacitinib citrate (540737-29-9) Tofacitinib citrate (CP-690550 citrate) (3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-1-piperidinepropanenitrile citrate CP-690550; TOFACITINIB; TASOCITINIB Xeljanz