Tofacitinib Powder CAS 477600-75-2
Product Name:Tofacitinib
CAS NO.:477600-75-2
Molecular Formula: C16H20N6O
Synonym:CP 690550;Tofacitinib CP690550 Tasocitinib;Tofacitinib citrate;CP 690550 Tofacitinib;CP-690550;Tasocitinib;Tasocitinib-CP690550;Tofacitinib;Tofacitinib (CP-690550,Tasocitinib);
Purity: Medicine grade 99%;Customizable
Test Method:HPLC/UV
MOQ & Package: 10g,100g,1kg etc Sub-package
Certificate:FDA,ISO,COA, HPLC, MSDS,TDS etc
Lead Time: 1-3 days
Shipping: DHL,Germany DHL,Germany DPD,UPS,USPS,FedEx,EMS,By Air,By Sea etc
Store & Shelf life; Cool & dry place;36 months
Other:There are warehouses in the United States, Australia and Germany.
Description
tofacitinib citrate is a Janus kinase inhibitor developed by Pfizer, USA, and its main component is pure Tasocitinib. It can be used for the treatment of moderate to severe active rheumatoid arthritis (RA) adult patients who have insufficient response or intolerance to methotrexate treatment. The Tofacitinib powder is off-white or light-colored raw material , and the finished product is a white round film-coated tablet with the words "Pfizer" on one side and "JKI5" on the other side, which is white to white-like after the coating is removed. On November 6, 2012, the US Food and Drug Administration (FDA) approved the substance to be marketed as a drug.
|
Tests |
Specifications |
Results |
|
Appearance |
White to off-white powder |
Off-white powder |
|
Identification |
A.IR:similar to Reference Substance |
Complies |
|
B.Retention Time:similarto Reference Substance |
Complies |
|
|
Loss on Drying |
≤0.5% |
0.12% |
|
Related substances |
Acetyl impurity≤0.15% |
Undetected |
|
Chloroacetyl impurity≤0.15% |
Undetected |
|
|
Diastereomer≤0.15% |
Undetected |
|
|
Single impurity≤0.10% |
0.03% |
|
|
Total impurities≤1.0% |
0.08% |
|
|
Enantiomer |
<0.15% |
0.07% |
|
Residual solvents |
Methanol≤3000ppm |
Undetected |
|
Toluene≤890ppm |
30ppm |
|
|
Ethanol<5000ppm |
595ppm |
|
|
Acetone≤5000ppm |
Undetected |
|
|
Dichloromethane≤600ppm |
Undetected |
|
|
Ethyl acetate<5000ppm |
192ppm |
|
|
Hexane<290ppm |
Undetected |
|
|
Assay |
98.0%-102.0%(Calculated on the dried basis) |
100.8% |
| Conclusion | Meets the Requirements |
Which is better, Upadacitinib or Tofacitinib?
Ankylosing spondylitis is a chronic immune disease with sacroiliac joint damage; Oral preparations of JAK1 inhibitors upatinib and tofatib have good effects on ankylosing spondylitis:
1.What is ankylosing spondylitis?
Ankylosing spondylitis is a chronic immune disease characterized by damage to the sacroiliac joints. The most common symptom is inflammatory lower back pain, which affects the spine and sacroiliac joints. As the disease progresses, it can cause spinal rigidity, difficulty in movement, and varying degrees of damage to multiple organ systems such as the eyes, lungs, cardiovascular system, and kidneys.
2.Effect of Tofacitinib
Tofacitinib powder is a JAK kinase inhibitor and a routine product used to treat rheumatoid arthritis. On November 6, 2020, Pfizer announced the positive results of a phase III clinical trial (A3921120) of oral JAK inhibitor tofacitinib in adult patients with active ankylosing spondylitis.
A3921120 is a multicenter, double-blind, placebo-controlled phase 3 study. The results showed that the study achieved the primary endpoint: at week 16 of treatment, the proportion of patients in the tofacitinib treatment group who achieved ASAS20 response significantly increased compared to the placebo group (56.4% vs 29.4%). In addition, compared with the placebo group, the proportion of patients who achieved ASAS40 response significantly increased in the tofacitinib treatment group (40.6% vs 12.5%).
3.Effect of Upatinib (UPA)
Upadacitinib powder is a selective JAK1 inhibitor that has shown good efficacy in clinical trials for the treatment of various autoimmune and inflammatory diseases. In 2019, Upatinib was launched in the United States and approved for the treatment of patients with moderate to severe rheumatoid arthritis. Shortly thereafter, the drug submitted a new indication application for ankylosing spondylitis.
The application for a new indication of Upatinib in the treatment of adult patients with active ankylosing spondylitis is supported by data from the SELECT-AXIS 1 study. SELECT-AXIS 1 is a multicenter, randomized, double-blind, parallel group, placebo-controlled, phase II/III study conducted in adult patients with active ankylosing spondylitis who have never received biologic modified antirheumatic drug therapy (bDMARD naive) and have insufficient response to at least two nonsteroidal anti-inflammatory drugs or are intolerant or contraindicated to nonsteroidal anti-inflammatory drugs.
The results showed that compared with placebo, Upatinib significantly improved the symptoms and signs of active AS in adult patients, and the proportion of patients who reached ASAS40 (International Society of Spinal Arthritis assessed improvement of 40%) at week 14 of treatment doubled (52% vs 26%).
4.Effect of Secukinumab
Secukinumab can selectively bind cytokine interleukin 17a (IL 17a) and inhibit the interaction with interleukin 17 receptor. On April 28th, 2020, Novartis Pharmaceutical (China) announced that Secukinumab was approved by National Medical Products Administration for ankylosing spondylitis.
MEASURE 5 is a China-centered, randomized, double-blind, placebo-controlled, parallel-group, multi-center and 52-week phase III clinical study. According to the results of this study, among all China patients treated with Secukinumab150mg, the response rate of ASAS20 has been significantly different from that of placebo group after 1 week of treatment; There was a significant difference in ASAS40 response rate after 2 weeks of treatment. After 16 weeks of treatment, the response rates of ASAS20/40 in Secukinumab group were 56.0% and 41.7% respectively, while those in placebo group were 38.5% and 16.5% respectively.
5.Comparison of therapeutic effects of Upadacitinib, Tofacitinib and Secukinumab on AS
|
Product |
Treatment time |
Reach the proportion of ASAS20(%) |
Reach the proportion of ASAS40(%) |
|
Upadacitinib |
14 weeks |
/ |
52% |
|
Tofacitinib |
16 weeks |
56.4% |
40.6% |
|
Secukinumab |
16 weeks |
56.0% |
41.7% |
Our company can provide a variety of JAK inhibitors. Besides tofacitinib and upatinib mentioned in this article, we can also provide products such as Baricitinib and Ruxolitinib. If you are interested, please leave a message by email:sales6@faithfulbio.com
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| 477600-75-2 tofacitinib | 1310726-60-3 upatinib/Upadacitinib | 1187594-09-7 Baricitinib | 941678-49-5 Ruxolitinib |
What are the therapeutic advantages of tofacitinib?
Tofacitinib powder can effectively inhibit the activity of JAK1 and JAK3, block the signal transduction of various inflammatory cytokines, and then inhibit the occurrence and development of inflammation, thus relieving joint pain, swelling and other symptoms. Compared with other drugs for treating autoimmune diseases such as rheumatoid arthritis, Tasocitinib powder has the following advantages: 1) As a selective inhibitor of JAK, it regulates cell autoimmunity by regulating JAK/STATs signal transduction pathway mediated by Type I/II cytokine receptors, and has good selectivity for autoimmune diseases; 2) As a small molecular compound, it has the characteristics of rapid onset. Oral administration can not only avoid unknown adverse reactions caused by other administration methods, but also continuously control the progress of the disease during the treatment. 3) Single administration or combined administration with non-biological agents such as methotrexate is effective.
A variety of shipping methods for you to choose
|
Transportation Time |
Shipping method |
Cargo weight requirements |
Advantage |
|
3-7 days |
DHL,Germany DHL,Germany DPD, |
Suitable for under 50kg. |
We have warehouses in Germany and California, USA, |
|
7-15 days |
By Air |
Suitable for more than 50kg. |
|
|
15-60 days |
By Sea |
Suitable for more than 500kg. |
Our strengths:
Our company has passed FDA and ISO19001 quality management system certification. And we have internal cooperation agreements with multiple factories and laboratories in China,Can provide you with a good price.If you are interested in tofacitinib,Upadacitinib,Baricitinib and Ruxolitinib ……other JAK suppression raw materials, please let us know.
We not only have unique advantages in transportation, but also support multiple payment methods, whether you use US dollars, euros, Australian dollars, or local currencies from Singapore, Malaysia, Thailand, and so on. We can also support local currencies in these regions and countries. In addition, we also support bank cards (credit cards, etc.) for payments.
Disclaimer: The information published on this website comes from the internet, which does not mean that this website agrees with its views or confirms the authenticity of the content. Please pay attention to distinguish it. In addition, the products provided by our company are only used for scientific research. We are not responsible for the consequences of any improper use.
If you are interested in our products, or have critical suggestions on our articles or are not completely satisfied with the products received, please contact us by Email :sales6@faithfulbio.com . Our team is committed to ensuring the complete satisfaction of customers.
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