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CGP77675 hydrate

Catalog No. T30855L

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 ( 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 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. CGP77675 hydrate can be useful for the treatment of diseases associated with elevated bone loss and has anticancer activity[1].

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

CGP77675 hydrate, CAS N/A

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 1,520.00
50 mg	10-14 weeks	$ 1,980.00
100 mg	10-14 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description	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 ( 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 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. CGP77675 hydrate can be useful for the treatment of diseases associated with elevated bone loss and has anticancer activity[1].
In vitro	CGP77675 hydrate effectively suppresses phosphorylation of poly-Glu-Tyr and the optimal Src substrate (OSS) peptide with IC50 values of 5.5 nM and 16.7 nM, respectively, aligning closely with chicken Src inhibition (20 nM). It also prevents parathyroid hormone-driven bone resorption in rat fetal long bone cultures at a 0.8 μM IC50. In IC8.1 cells exhibiting Src overexpression, CGP77675 hydrate (0.04-10 μM; 2 hours) significantly reduces tyrosine phosphorylation of Src substrates Fak and paxillin with IC50 values of 0.2 and 0.5 μM, respectively, while having a lesser impact on Src itself (5.7 μM). Viability tests on MC3T3-E1 cells treated with 0.2, 1, and 5 μM for three days show no adverse effects on cell health. Additionally, western blot analysis reveals a dose-dependent inhibition of Fak and paxillin phosphorylation without affecting Src in Src-overexpressing IC8.1 cells.
In vivo	CGP77675 hydrate administered subcutaneously at dosages of 1, 5, and 25 mg/kg twice daily effectively inhibits interleukin-1β (IL-1β)-induced hypercalcemia in male mice (Tif:MAGf; Novartis Animal Farm) weighing 25-30 g, without impacting serum amyloid protein levels [1]. Additionally, when given orally at doses of 10 and 50 mg/kg twice daily for six weeks to eight-week-old female Sprague-Dawley-derived Tif:RAlf rats (175-209 g), it partially prevents bone loss and improves bone microarchitecture in young ovariectomized (ovx) rats, showcasing its potential in preserving bone health [1].

Molecular Weight

N/A

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CGP77675 hydrate CGP77675 Hydrate CGP 77675 Hydrate CGP-77675 hydrate CGP-77675 Hydrate inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.