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CGP77675

CAS No. : 234772-64-6

MCE 站：CGP77675

产品活性：CGP77675 是一种有效的 Src 家族激酶抑制剂。CGP77675 抑制 Src，EGFR，KDR，v-Abl 和 Lck，IC₅₀ 分别为 0.02、0.15、1.0、0.31 和 0.29 μM。具有抗肿瘤活性。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Src

In Vitro: CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC₅₀s of 5-20 and 40 nM, respectively) .
CGP77675 dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC₅₀ value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC₅₀ value of 16.7 nM. These IC₅₀ values are similar to the value obtained with chicken Src (20 nM).
CGP77675 inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC₅₀ of 0.8 μM.
CGP77675 (0.04-10 μM; 2 hours) potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin, but has much less effect on Src (IC₅₀ values 0.2, 0.5, and 5.7μM) in IC8.1 cells.

In Vivo: CGP77675 (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice.
CGP77675 (10 and 50 mg/kg; administered orally; twice a day for 6 weeks) partially prevents bone loss and rescues bone microarchitectural features in young ovx rats.

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