Description In vitro In vivo References
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Tofacitinib citrate

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

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
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Safety

WGK Germany 
3
HS Code 
29335990
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PZ0017
Product name
Tofacitinib citrate
Purity
≥98% (HPLC)
Packaging
5mg
Price
$106
Updated
2021/03/22
Sigma-Aldrich
Product number
PZ0017
Product name
Tofacitinib citrate
Purity
≥98% (HPLC)
Packaging
25mg
Price
$423
Updated
2021/03/22
Cayman Chemical
Product number
11598
Product name
CP 690,550
Purity
≥98%
Packaging
5mg
Price
$55
Updated
2021/03/22
Cayman Chemical
Product number
11598
Product name
CP 690,550
Purity
≥98%
Packaging
10mg
Price
$105
Updated
2021/03/22
Cayman Chemical
Product number
11598
Product name
CP 690,550
Purity
≥98%
Packaging
25mg
Price
$206
Updated
2021/03/22
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Tofacitinib citrate Chemical Properties,Usage,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

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Tofacitinib citrate Suppliers

Shanghai Boc Chemical Co.,Ltd
Tel
021-34975603-808
Fax
+86-21-34975602-805
Email
sales@bocpharma.com
Country
China
ProdList
932
Advantage
64
Zhuhai Yourun Co., Ltd.
Tel
0756-6811852-
Fax
0756-6811857
Email
zhuhaiyourun@126.com
Country
China
ProdList
126
Advantage
55
Junyu Chemexpress Co., Ltd.
Fax
0731-88036271
Email
info@csjyyy.cn
Country
China
ProdList
30
Advantage
58
Cangzhou Enke Pharma-tech Co., Ltd.
Tel
0317-5296180-
Fax
0317-5106596
Email
sale@enkepharma.com
Country
China
ProdList
866
Advantage
55
Shanghai jing Hao pharmaceutical technology co., LTD
Tel
Fax
021-68900963
Email
sales@jinghaopharma.com
Country
China
ProdList
199
Advantage
58
Nanjing Wedo Pharm Tech Co., Ltd.
Tel
Email
190644657@qq.com
Country
China
ProdList
224
Advantage
58
Gansu HaoTian Chemical Technology Co., Ltd.
Tel
0931-8238232-
Fax
0931-8238232
Email
shijiaowang@haotianpharm.com
Country
China
ProdList
94
Advantage
55
Shandong Sihuan Pharmaceutical Co., Ltd.
Tel
0531-88990215- ;0531-88993983-
Fax
QQ:195229932
Email
melissa@sdsihuanpharm.com;debby@sdsihuanpharm.com
Country
China
ProdList
63
Advantage
58
Beijing Huikang Boyuan Chemical Tech Co., Ltd
Tel
010-68862197
Fax
010-68882204
Email
bjhkby@126.com
Country
China
ProdList
110
Advantage
61
Shanghai Boyle Chemical Co., Ltd.
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2926
Advantage
55
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View Lastest Price from Tofacitinib citrate manufacturers

Wuhan wingroup Pharmaceutical Co., Ltd
Product
Tofacitinib citrate 540737-29-9
Price
US $10.00/KG
Min. Order
1KG
Purity
99.9%
Supply Ability
100MT/Month
Release date
2021-07-06
WUHAN FORTUNA CHEMICAL CO., LTD
Product
Tofacitinib citrate 540737-29-9
Price
US $0.00-0.00/g
Min. Order
1g
Purity
99%min
Supply Ability
1000G
Release date
2021-07-17
Anhui Rencheng Technology Co., Ltd
Product
Tofacitinib Citrate 540737-29-9
Price
US $5.00-15.00/KG
Min. Order
0.5KG
Purity
>99%
Supply Ability
20tons
Release date
2020-12-28

540737-29-9, Tofacitinib citrateRelated Search:


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