TC-S 7003

Research use only, not for human use.

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.

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.

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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.

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Angiogenesis

Syk

Syk | Src

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847950-09-8

530.62

C31H30N8O

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (188.46 mM; Ultrasonic )

O=C1C2=CN=C(N=C2N3C(=NC=4C=CC=CC43)N1C=5C(=CC=CC5C)C)NC6=CC=C(C=C6)N7CCN(C)CC7

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(-20℃)

With Ice Pack

≥ 2 years