货号 | 15135-1mg |
描述 | Lymphocyte-specific protein tyrosine kinase (Lck) is a member of the Src-family of non-receptor protein tyrosine kinases and plays a critical role in the initial steps of T cell receptor signaling that trigger the production of cytokines.1 Lck inhibitor is a pyrrolopyrimidine that blocks the activity of two forms of Lck kinase, Lck (64-509) and Lckcd, with IC50 values of <1 and 2 nM, respectively.2,3 It inhibits the related kinases Src, Kdr, and Tie-2 with much weaker potency (IC50s = 70 nM, 1.57, and 1.98 µM, respectively) and only minimally inhibits the activities of EGFR, PKC, CDC2/B and ZAP-70 (IC50s = 3.2, >33, >50, and >50 µM, respectively).2,3 This compound has been shown to inhibit T cell receptor-stimulated IL-2 production in mice (ED50s = 4 and 25 mg/kg when administered either i.p. or orally).2,4 |
别名 | Lymphocyte-specific protein tyrosine kinase;RK-24466; |
供应商 | Cayman |
应用文献 | |
1.Khatik, R. and Pathak, A.K. Lck inhibitors and its analogues: A review. Der Pharma Chemica 3(2), 310-320 (2011). 2.Burchat, A.F.,Calderwood, D.J.,Hirst, G.C., et al. Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II. Bioorganic & Medicinal Chemistry Letters 10(19), 2171-2174 (2000). 3.Arnold, L.D.,Calderwood, D.J.,Dixon, R.W., et al. Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. Bioorganic & Medicinal Chemistry Letters 10(19), 2167-2170 (2000). 4.Calderwood, D.J.,Johnston, D.N.,Munschauer, R., et al. Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck. Bioorganic & Medicinal Chemistry Letters 12(12), 1683-1686 (2002). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 370.5 |
分子式 | C23H22N4O |
CAS号 | 213743-31-8 |
稳定性 | ≥ 2 years |
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