CGP77675
Based on 1 Customer Validation
CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 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 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.46%
- No. CAS: 234772-64-6
- Fòrmula: C26H29N5O2
- Peso molecular:443.54
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Almacenamiento:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)[1]
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)[1].
CGP77675 inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC50 of 0.8 μM[1].
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[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 (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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No. CAS 234772-64-6
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Appearance Solid
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Peso molecular 443.54
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Fòrmula C26H29N5O2
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Color White to light yellow
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvente y solubilidad
DMSO : 26.0 mg/mL (58.62 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2546 mL | 11.2729 mL | 22.5459 mL | 56.3647 mL |
| 5 mM | 0.4509 mL | 2.2546 mL | 4.5092 mL | 11.2729 mL | |
| 10 mM | 0.2255 mL | 1.1273 mL | 2.2546 mL | 5.6365 mL | |
| 15 mM | 0.1503 mL | 0.7515 mL | 1.5031 mL | 3.7576 mL | |
| 20 mM | 0.1127 mL | 0.5636 mL | 1.1273 mL | 2.8182 mL | |
| 25 mM | 0.0902 mL | 0.4509 mL | 0.9018 mL | 2.2546 mL | |
| 30 mM | 0.0752 mL | 0.3758 mL | 0.7515 mL | 1.8788 mL | |
| 40 mM | 0.0564 mL | 0.2818 mL | 0.5636 mL | 1.4091 mL | |
| 50 mM | 0.0451 mL | 0.2255 mL | 0.4509 mL | 1.1273 mL |
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