CGP77675 是一种口服有效的 Src 家族激酶抑制剂。CGP77675 抑制肽底物的磷酸化和纯化 Src 的自磷酸化 (IC₅₀ 分别为 5-20 和 40 nM)，并且还抑制 Src，EGFR，KDR，v-Abl 和 Lck，IC₅₀ 分别为 20、150、1000、310 和 290 nM。具有抗肿瘤活性。

CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC 50 s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC 50 s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity.

Solid

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

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

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

Room temperature in continental US; may vary elsewhere.

-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[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.

In Vitro: DMSO : 26.0 mg/mL (58.62 mM; Need ultrasonic and warming)配制储备液