CGP77675 hydrate 

CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC₅₀s of 5-20 and 40 nM, respectively),and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC₅₀s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity^[1].

IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)^[1]

CGP77675 hydrate 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)^[1].
CGP77675 hydrate inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC₅₀ of 0.8 μM^[1].
CGP77675 hydrate (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^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CGP77675 hydrate (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice^[1].
CGP77675 hydrate (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^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

C₂₆H₂₉N₅O₂.xH₂O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Missbach M, et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellularsubstrates and reduces bone resorption in vitro and in rodent models in vivo. Bone. 1999 May;24(5):437-49.  [Content Brief]