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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C26H29N5O2.xH2O
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
化学情報
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CGP77675 hydrate 関連分類
HY-W062835A 関連分類
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