CGP77675

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CGP77675 是一种有效的选择性 Src 家族激酶抑制剂，对肽底物的磷酸化和纯化的 Src 的自磷酸化的 IC50 为 5-20 和 40 nM。 CGP77675 具有抗癌活性。

CGP77675 is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylation of purified Src. CGP77675 exhibits anticancer activity.(In Vitro):CGP77675 inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 20, 150, 1000, 310, and 290 nM, respectively. CGP77675 dose-dependently inhibits phosphorylation of poly-Glu-Tyr (IC50 = 5.5 nM), and of the optimal Src substrate (OSS) peptide (IC50 = 16.7 nM). In rat fetal long bone cultures, CGP77675 inhibits the parathyroid hormone-induced bone resorption (IC50 = 0.8 μM). In Src-overexpressing IC8.1 cells, CGP77675 (0.04-10 μM) dose-dependently inhibits phosphorylation of Fak (IC50 = 0.2 μM) and paxillin(IC50 = 0.5 μM), but not of Src(IC50 = 5.7μM).(In Vivo):In female rats of the Sprague-Dawley-derived strain Tif:RAlf, CGP77675 (10 and 50 mg/kg;orally) partially prevents bone loss and rescues bone microarchitectural features. In male mice, CGP77675 (1, 5, and 25 mg/kg; s.c.) inhibits IL-1β-induced hypercalcemia without affecting serum amyloid protein levels.

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.Cell Viability Assay Cell Line:MC3T3-E1 cells Concentration:0.2, 1, and 5 μM Incubation Time:3 days Result:Did not influence cell viability for up to 3 days of treatment.Western Blot Analysis Cell Line:Src-overexpressing IC8.1 cells Concentration:0.04, 0.2, 1, 5, and 10 μM Incubation Time:2 hours Result:Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src.

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. Animal Model:Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body Dosage:1, 5, and 25 mg/kg Administration:Injected s.c.; twice a day Result:Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels. Animal Model:Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf Dosage:10 and 50 mg/kg Administration:Administered orally; twice a day for 6 weeks Result:Partly prevented bone loss.

CGP-77675 | CGP 77675 | 1-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol | ZINC1488120

Angiogenesis

EGFR

TNAP

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234772-64-6

443.54

C26H29N5O2

>98% (HPLC)

In Vitro:?DMSO : 26.0 mg/mL (58.62 mM)

OC1CCN(CCC2=CC=C(C=C2)N3C=C(C=4C=CC=C(OC)C4)C=5C(=NC=NC53)N)CC1

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(-20℃)

With Ice Pack

≥ 2 years