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MedKoo CAT#: 200811

CAS#: 477600-75-2 (free base)

Description: Tofacitinib, also known as tasocitinib, CP-690550, is a Janus kinase (JAK) inhibitor. Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs. JAK enzymes transmit cytokine signaling through pairing of JAKs (e.g., JAK1/JAK3, JAK1/JAK2, JAK1/TyK2, JAK2/JAK2). Tofacitinib inhibited the in vitro activities of JAK1/JAK2, JAK1/JAK3, and JAK2/JAK2 combinations with IC50 of 406, 56, and 1377 nM, respectively.

Price and Availability

Size Price Shipping out time Quantity
100mg USD 90 Same day
200mg USD 150 Same day
500mg USD 250 Same day
1g USD 450 Same day
2g USD 850 Same day
5g USD 1750 Same day
10g USD 2850 Same day
20g USD 4250 Same day
100g USD 8950 Same day
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Pricing updated 2020-08-11. Prices are subject to change without notice.

Tofacitinib free base, purity > 98%, is in stock. The same day shipping out after order is received.

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 200811
Name: Tofacitinib
CAS#: 477600-75-2 (free base)
Chemical Formula: C16H20N6O
Exact Mass: 312.16986
Molecular Weight: 312.37
Elemental Analysis: C, 61.52; H, 6.45; N, 26.90; O, 5.12

Related CAS #: 540737-29-9 (citrate)   477600-75-2 (free base)    

Synonym: Tofacitinib free base; CP690550; CP-690550; CP 690550; Tofacitinib. Trade name Xeljanz

IUPAC/Chemical Name: 3-((3R,4R)-4-Methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile


InChi Code: InChI=1S/C16H20N6O/c1-11-5-8-22(14(23)3-6-17)9-13(11)21(2)16-12-4-7-18-15(12)19-10-20-16/h4,7,10-11,13H,3,5,8-9H2,1-2H3,(H,18,19,20)/t11-,13+/m1/s1

SMILES Code: N#CCC(N1C[C@H](N(C)C2=C3C(NC=C3)=NC=N2)[C@H](C)CC1)=O

Technical Data

White to off-white solid powder

>98% (or refer to the Certificate of Analysis)

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Soluble in DMSO (15mg/ mL)

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:

Additional Information

It is an inhibitor of the enzyme janus kinase 3 (JAK3), which means that it interferes with the JAK-STAT signaling pathway, which transmits extracellular information into the cell nucleus, influencing DNA transcription. Recently it has been shown in a murine model of established arthritis that tofacitinib rapidly improved disease by inhibiting the production of inflammatory mediators and suppressing STAT1-dependent genes in joint tissue. This efficacy in this disease model correlated with the inhibition of both JAK1 and 3 signaling pathways, suggesting that tofacitinib may exert therapeutic benefit via pathways that are not exclusive to inhibition of JAK3.


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2: Papp KA, Krueger JG, Feldman SR, Langley RG, Thaci D, Torii H, Tyring S, Wolk R, Gardner A, Mebus C, Tan H, Luo Y, Gupta P, Mallbris L, Tatulych S. Tofacitinib, an oral Janus kinase inhibitor, for the treatment of chronic plaque psoriasis: Long-term efficacy and safety results from 2 randomized phase-III studies and 1 open-label long-term extension study. J Am Acad Dermatol. 2016 May;74(5):841-50. doi: 10.1016/j.jaad.2016.01.013. PubMed PMID: 26899199.

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13: Fleischmann R, Mease PJ, Schwartzman S, Hwang LJ, Soma K, Connell CA, Takiya L, Bananis E. Efficacy of tofacitinib in patients with rheumatoid arthritis stratified by background methotrexate dose group. Clin Rheumatol. 2017 Jan;36(1):15-24. doi: 10.1007/s10067-016-3436-1. PubMed PMID: 27734232; PubMed Central PMCID: PMC5216063.

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15: Vieira MC, Zwillich SH, Jansen JP, Smiechowski B, Spurden D, Wallenstein GV. Tofacitinib Versus Biologic Treatments in Patients With Active Rheumatoid Arthritis Who Have Had an Inadequate Response to Tumor Necrosis Factor Inhibitors: Results From a Network Meta-analysis. Clin Ther. 2016 Dec;38(12):2628-2641.e5. doi: 10.1016/j.clinthera.2016.11.004. PubMed PMID: 27889300.

16: Charles-Schoeman C, Wicker P, Gonzalez-Gay MA, Boy M, Zuckerman A, Soma K, Geier J, Kwok K, Riese R. Cardiovascular safety findings in patients with rheumatoid arthritis treated with tofacitinib, an oral Janus kinase inhibitor. Semin Arthritis Rheum. 2016 Dec;46(3):261-271. doi: 10.1016/j.semarthrit.2016.05.014. PubMed PMID: 27443588.

17: Strand V, Ahadieh S, French J, Geier J, Krishnaswami S, Menon S, Checchio T, Tensfeldt TG, Hoffman E, Riese R, Boy M, Gómez-Reino JJ. Systematic review and meta-analysis of serious infections with tofacitinib and biologic disease-modifying antirheumatic drug treatment in rheumatoid arthritis clinical trials. Arthritis Res Ther. 2015 Dec 15;17:362. doi: 10.1186/s13075-015-0880-2. Review. PubMed PMID: 26669566; PubMed Central PMCID: PMC4704538.

18: Strand V, Kremer J, Wallenstein G, Kanik KS, Connell C, Gruben D, Zwillich SH, Fleischmann R. Effects of tofacitinib monotherapy on patient-reported outcomes in a randomized phase 3 study of patients with active rheumatoid arthritis and inadequate responses to DMARDs. Arthritis Res Ther. 2015 Nov 4;17:307. doi: 10.1186/s13075-015-0825-9. PubMed PMID: 26530039; PubMed Central PMCID: PMC4632359.

19: Feldman SR, Thaçi D, Gooderham M, Augustin M, de la Cruz C, Mallbris L, Buonanno M, Tatulych S, Kaur M, Lan S, Valdez H, Mamolo C. Tofacitinib improves pruritus and health-related quality of life up to 52 weeks: Results from 2 randomized phase III trials in patients with moderate to severe plaque psoriasis. J Am Acad Dermatol. 2016 Dec;75(6):1162-1170.e3. doi: 10.1016/j.jaad.2016.07.040. PubMed PMID: 27692733.

20: Wu JJ, Strober BE, Hansen PR, Ahlehoff O, Egeberg A, Qureshi AA, Robertson D, Valdez H, Tan H, Wolk R. Effects of tofacitinib on cardiovascular risk factors and cardiovascular outcomes based on phase III and long-term extension data in patients with plaque psoriasis. J Am Acad Dermatol. 2016 Nov;75(5):897-905. doi: 10.1016/j.jaad.2016.06.012. PubMed PMID: 27498960.