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Tofacitinib citrate

Description In vitro In vivo References
Tofacitinib citrate
Tofacitinib citrate structure
CAS No.
540737-29-9
Chemical Name:
Tofacitinib citrate
Synonyms
CS-656;Xeljanz;CP 690500-10;CP 690550-10;Tofacitinib API;CP-690550 citrate;Tofacitnib Citrate;Tofacitinib citrate;Tasocitinib citrate;Tofacititinib cirate
CBNumber:
CB92460269
Molecular Formula:
C16H20N6O.C6H8O7
Formula Weight:
504.497
MOL File:
540737-29-9.mol

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
FDA UNII
O1FF4DIV0D
SAFETY
  • Risk and Safety Statements
WGK Germany  3
HS Code  29335990

Tofacitinib citrate price More Price(6)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich PZ0017 Tofacitinib citrate ≥98% (HPLC) 540737-29-9 5mg $97.3 2019-12-02 Buy
Sigma-Aldrich PZ0017 Tofacitinib citrate ≥98% (HPLC) 540737-29-9 25mg $393 2019-12-02 Buy
Cayman Chemical 11598 CP 690,550 ≥98% 540737-29-9 5mg $55 2020-06-24 Buy
Cayman Chemical 11598 CP 690,550 ≥98% 540737-29-9 10mg $99 2020-06-24 Buy
Cayman Chemical 11598 CP 690,550 ≥98% 540737-29-9 25mg $193 2020-06-24 Buy

Tofacitinib citrate Chemical Properties,Uses,Production

Description

Tofacitinib 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.

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.).

References

http://www.medicinenet.com/tofacitinib_citrate_xeljanz/article.htm

Definition

ChEBI: A citrate salt obtained by combining equimolar amounts of tofacitinib and citric acid. Used to treat moderately to severely active Rheumatoid Arthritis.

Tofacitinib citrate Preparation Products And Raw materials

Raw materials

Preparation Products


Tofacitinib citrate Suppliers

Global( 294)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597
sales03@yibaibiotech.com CHINA 420 58
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 296 58
Shanghai Jinghao Pharmaceutical Co.,Ltd
+86-21-68900963
+86-21-68900963 sales@jinghaopharma.com CHINA 127 58
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22626 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070
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ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24723 60
Shandonghaohong biotechnology Co.,ltd.
0635-6175299 13961496334
0635-6175299 sale@inyelchem.com CHINA 44 55
Hebei Chisure Biotechnology Co., Ltd.
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career henan chemical co
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View Lastest Price from Tofacitinib citrate manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-07-05 Tofacitinib citrate
540737-29-9
US $10.00 / KG 1KG 99% 10 mt Hebei Guanlang Biotechnology Co., Ltd.
2020-04-23 Tofacitinib citrate
540737-29-9
US $0.10 / KG 1KG 99.0% 1000 tons Shaanxi Dideu Medichem Co. Ltd
2019-12-26 Tofacitinib citrate
540737-29-9
US $0.10-0.10 / KG 1KG 99%+ 10000KG Shaanxi Dideu Medichem Co. Ltd

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