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.
For research use only. We do not sell to patients.
- Formula: C26H29N5O2.xH2O
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MC3T3-E1 cells
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Concentration:0.2, 1, and 5 μM
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Incubation Time:3 days
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Result:Did not influence cell viability for up to 3 days of treatment.
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Cell Line:Src-overexpressing IC8.1 cells
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Concentration:0.04, 0.2, 1, 5, and 10 μM
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Incubation Time:2 hours
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Result:Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body[1]
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Dosage:1, 5, and 25 mg/kg
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Administration:Injected s.c.; twice a day
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Result:Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels.
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Animal Model:Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf[1]
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Dosage:10 and 50 mg/kg
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Administration:Administered orally; twice a day for 6 weeks
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Result:Partly prevented bone loss.
Chemical Information
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Formula C26H29N5O2.xH2O
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SMILES
OC1CCN(CCC2=CC=C(N3C=C(C4=CC=CC(OC)=C4)C5=C(N)N=CN=C53)C=C2)CC1.O.[x]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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