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TC-S 7003

CAS No. 847950-09-8

TC-S 7003( —— )

Catalog No. M33407 CAS No. 847950-09-8

TC-S 7003 (Lck Inhibitor) is an orally active, selective and potent lymphocyte kinase (Lck) inhibitor with anti-inflammatory activity, inhibition of Lck, Lyn, Src, and Syk kinases, and inhibition of T-cell proliferation, and may be useful in the study of arthritis.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    TC-S 7003
  • Note
    Research use only, not for human use.
  • Brief Description
    TC-S 7003 (Lck Inhibitor) is an orally active, selective and potent lymphocyte kinase (Lck) inhibitor with anti-inflammatory activity, inhibition of Lck, Lyn, Src, and Syk kinases, and inhibition of T-cell proliferation, and may be useful in the study of arthritis.
  • Description
    Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
  • In Vitro
    ——
  • In Vivo
    Animal Model:Male Lewis rat (adjuvant-inducedarthritis model) Dosage:0, 30, and 60 mg/kg Administration:P.o.; once daily; from day 9 today 17 Result:Showed a dose-dependent inhibition of arthritis, with an ED50 estimated at 24 mg/kg.Animal Model:Sprague-Dawley Rats Dosage:P.o. (Pharmacokinetic Analysis) Administration:5 mg/kg Result:The Cmax, AUC0-∞, tmax and F% were 82 ng/mL, 862 ng h/mL, and 17%, respectively.
  • Synonyms
    ——
  • Pathway
    Angiogenesis
  • Target
    Syk
  • Recptor
    Syk | Src
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    847950-09-8
  • Formula Weight
    530.62
  • Molecular Formula
    C31H30N8O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (188.46 mM; Ultrasonic )
  • SMILES
    O=C1C2=CN=C(N=C2N3C(=NC=4C=CC=CC43)N1C=5C(=CC=CC5C)C)NC6=CC=C(C=C6)N7CCN(C)CC7
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Martin, Matthew W.; Newcomb, John; Nunes, Joseph J.; et al. Structure-Based Design of Novel 2-Amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as Potent and Orally Active Inhibitors of Lymphocyte Specific Kinase (Lck): Synthesis, SAR, and In Vivo Anti-Inflammatory Activity. Journal of Medicinal Chemistry (2008), 51(6), 1637-1648.?
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