Tasocitinib

Effective Anti Tumor Inhibitor API Tofacitinib Citrate
(CAS: 540737-29-9)
Chemical Information

Target	JAK3	JAK2	JAK1	ROCK2	LCK
IC50	1 nM	20 nM	112 nM	3.4 μM	3.87 μM

Product Name:	Tofacitinib Citrate
Other Names:	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);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...;Xeljanz;CP-690550 (Tofacitinib citrate)Other Names: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);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...;Xeljanz;CP-690550 (Tofacitinib citrate)
CAS No.:	540737-29-9
MF:	C16H20N6O.C6H8O7
MW:	504.497
Appearance:	White or Nearly White Crystalline Powder
Purity:	99%+
Specifications:	Pharmaceutical Grade
MOQ):	10g
Packing:	Aluminium Foil Bag or as Required

Product Description

Tofacitinib (formerly tasocitinib, CP-690550) is a drug being investigated for the treatment of rheumatoid arthritis (RA), psoriasis, inflammatory bowel disease, and other immunological diseases, as well as for the prevention of organ transplant rejection. It is an inhibitor of the enzyme Janus kinase 3 (JAK3), which means that it interferes with the JAK-STAT signaling pathway that transmits information outside the cell into the cell nucleus, influencing DNA transcription. Recently it has been shown in a murine model of established arthritis, 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.

Applications/Usage
A concentration of 100 nM. 50 nM, but not 10 nM, CP-690,550 suppressed IFN- c production 4 days after Th1 differentiation conditions were established, while both 10 nM and 50 nM CP-690,550 strongly suppressed IL-4 production under Th2 differentiation conditions. This suggests that CP-690,550 inhibits both Th1 and Th2 differentiation, and that Th2 is more sensitive than Th1 to this drug. We then examined the effect of CP-690,550 on Th17 and induced T regulatory (iTreg) cells. CP-690,550 enhanced IL-17 production while suppressing Foxp3 and IL-10 induction in a dose-dependent manner under Th17 differentiation conditions. These data indicate that <100 nM CP-690,550 efficiently inhibits Th1, Th2 and iTreg while promoting Th17, in vitro.

Tofacitinib citrate is currently approved for the treatment of rheumatoid arthritis.Tofacitinib citrate is an inhibitor of the enzyme janus kinase 3.
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