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CP-690550, JAK Inhibitor

CP-690550, JAK Inhibitor

$79.00
A potent and selective pan-JAK Inhibitor in clinical trials for rheumatoid arthritis.
Catalog No. Unit Price Qty
M60033-2s 2 mg solid $79.00
M60033-2 10 mM in DMSO (0.641 mL) $79.00
M60033-25s 25 mg solid $550.00

Details

Product Information
Chemical Name: 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile
Molecular Weight: 312.38
Formula: C16H20N6O
Purity: ≥ 98%
CAS#: 477600-75-2
Solubility: DMSO up to 100 mM
Storage: Powder: 4oC 1 year DMSO: 4oC 3 month -20oC 1 year

Biological Activity:

CP-690550 is a potent and selective JAK inhibitor currently in clinical trials for rheumatoid arthritis (RA) and other autoimmune disease indications.  It inhibits recombinant human JAK1 (IC50 ~ 3.2 nM), JAK2 (IC50 ~4.1 nM), and JAK3 (IC50 ~1.6 nM). In cellular assays CP-690550 showed potent effects in the IL-2 blast proliferation assay (IC50 ~11 nM, mediated via JAK1 and JAK3) and HU03 cellular specificity assay (IC50 ~324 nM, mediated via JAK2), but has relatively minimal effects on general cell growth (>10 µM activity in the HFF assay).


How to Use:

  • In vitro:  CP-690550 was used at 0.05-1 µM concentration in a panel of in vitro assays.
  • In vivo: CP-690550 was orally dosed to rats at 10-50 mg/kg once or twice per day.


Reference:

  1. 1.  Flanagan ME, et al. Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection. (2010) J Med Chem. 53(24):8468-84
  2. 2.  Meyer DM, et al. Anti-inflammatory activity and neutrophil reductions mediated by the JAK1/JAK3 inhibitor, CP-690,550, in rat adjuvant-induced arthritis. (2010) J Inflamm (Lond).11;7:41.
  3. 3.  Ghoreschi K, et al. Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550). (2011) J Immunol. 186(7):4234-43.
  4. 4.  Ju W, et al. CP-690,550, a therapeutic agent, inhibits cytokine-mediated Jak3 activation and proliferation of T cells from patients with ATL and HAM/TSP. (2011) Blood. 117(6):1938-46.



Products are for research use only. Not for human use.

Description

Details

Product Information
Chemical Name: 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile
Molecular Weight: 312.38
Formula: C16H20N6O
Purity: ≥ 98%
CAS#: 477600-75-2
Solubility: DMSO up to 100 mM
Storage: Powder: 4oC 1 year DMSO: 4oC 3 month -20oC 1 year

Biological Activity:

CP-690550 is a potent and selective JAK inhibitor currently in clinical trials for rheumatoid arthritis (RA) and other autoimmune disease indications.  It inhibits recombinant human JAK1 (IC50 ~ 3.2 nM), JAK2 (IC50 ~4.1 nM), and JAK3 (IC50 ~1.6 nM). In cellular assays CP-690550 showed potent effects in the IL-2 blast proliferation assay (IC50 ~11 nM, mediated via JAK1 and JAK3) and HU03 cellular specificity assay (IC50 ~324 nM, mediated via JAK2), but has relatively minimal effects on general cell growth (>10 µM activity in the HFF assay).


How to Use:

  • In vitro:  CP-690550 was used at 0.05-1 µM concentration in a panel of in vitro assays.
  • In vivo: CP-690550 was orally dosed to rats at 10-50 mg/kg once or twice per day.


Reference:

  1. 1.  Flanagan ME, et al. Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection. (2010) J Med Chem. 53(24):8468-84
  2. 2.  Meyer DM, et al. Anti-inflammatory activity and neutrophil reductions mediated by the JAK1/JAK3 inhibitor, CP-690,550, in rat adjuvant-induced arthritis. (2010) J Inflamm (Lond).11;7:41.
  3. 3.  Ghoreschi K, et al. Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550). (2011) J Immunol. 186(7):4234-43.
  4. 4.  Ju W, et al. CP-690,550, a therapeutic agent, inhibits cytokine-mediated Jak3 activation and proliferation of T cells from patients with ATL and HAM/TSP. (2011) Blood. 117(6):1938-46.



Products are for research use only. Not for human use.

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