A covalent JAK3 inhibitor
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

PF-06651600

Item No. 21054

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(2S,5R)-2-methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one
CAS Number
1792180-81-4
Synonyms
  • Ritlecitinib
Molecular Formula
C15H19N5O
Formula Weight
285.3
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleDMSO: Soluble
SMILES
O=C(C=C)N(C1)[C@@H](C)CC[C@@H]1NC2=C3C(NC=C3)=NC=N2
InChi Code
InChI=1S/C15H19N5O/c1-3-13(21)20-8-11(5-4-10(20)2)19-15-12-6-7-16-14(12)17-9-18-15/h3,6-7,9-11H,1,4-5,8H2,2H3,(H2,16,17,18,19)/t10-,11-/m0/s1
InChi Key
CBRJPFGIXUFMTM-QWRGUYRKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products
Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    10 mg

    $91

    Add

    50 mg

    $429

    Add

    100 mg

    $767

    Add

    250 mg

    $1,241

    Add
    Kinase Resource Center
    Discover Products & Resources for Kinase Research
    • Kinase inhibitors, screening libraries, assay kits, & more
    • Tools to study kinase signaling pathways:
      • Growth factor signaling
      • PI3K/Akt/mTOR
      • MAPKs (ERK, p38, & JNK)
      • JAK/STAT signaling
    • Articles, resources, & advice
    EXPLORE NOW
    Product Description

    PF-06651600 is a covalent inhibitor of JAK3 (IC50 = 33.1 nM).1 It is selective for JAK3 over JAK1, JAK2, and tyrosine kinase 2 (TYK2; IC50s = >10,000 for all) and a panel of 304 other kinases at 1 µM. PF-06651600 inhibits STAT5, STAT6, and STAT3 phosphorylation induced by IL-2, IL-4, or IL-21, respectively, in isolated human lymphocytes (IC50s = 244, 340, and 350 nM, respectively). It inhibits T cell differentiation into the T helper cells Th1 and Th17 in a T cell differentiation assay (IC50s = 30 and 167 nM, respectively). PF-06651600 (3, 10, or 30 mg/kg) reduces paw swelling in a rat model of adjuvant-induced arthritis. It also decreases disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at doses of 30 or 100 mg/kg. Formulations containing PF-06651600 have been used in the treatment of severe alopecia in adults and adolescents.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Telliez, J.-B., Dowty, M.E., Wang, L., et al. Discovery of a JAK3-selective inhibitor: Functional differentiation of JAK3-selective inhibition over pan-JAK or JAK1-selective inhibition. ACS Chem. Biol. 11(12), 3442-3451 (2016).