| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)[1]
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|---|---|
| ln Vitro |
At an IC50 of 5.5 nM for poly-Glu-Tyr and 16.7 nM for the optimal Src substrate (OSS) peptide, CGP77675 hydrate inhibits phosphorylation of both in a dose-dependent manner. Similar results were obtained using chicken Src (20 nM)[1], as indicated by these IC50 values. With a half-life of 0.8 micrometers, CGP77675 hydrate prevents bone resorption brought on by parathyroid hormone in rat fetal long bone cultures[1]. Src substrates Fak and paxillin are significantly less susceptible to CGP77675 hydrate (0.04-10 μM; 2 hours) than Src (IC50 values 0.2, 0.5, and 5.7 μM) in IC8.1 cells.
|
| ln Vivo |
CGP77675 hydrate (given subcutaneously, s.c., twice daily at 1, 5, and 25 mg/kg) prevents IL-1β-induced hypercalcemia in mice[1]. In young ovx rats, CGP77675 hydrate (10 and 50 mg/kg; given orally; twice daily for 6 weeks) recovers bone microarchitectural characteristics and largely prevents bone loss[1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: MC3T3-E1 cells Tested Concentrations: 0.2, 1, and 5 μM Incubation Duration: 3 days Experimental Results: Did not influence cell viability for up to 3 days of treatment. Western Blot Analysis[1] Cell Types: Src-overexpressing IC8.1 cells Tested Concentrations: 0.04, 0.2, 1, 5, and 10 μM Incubation Duration: 2 hrs (hours) Experimental Results: Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src. |
| Animal Protocol |
Animal/Disease Models: Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body[1]
Doses: 1, 5, and 25 mg/kg Route of Administration: Injected sc; twice a day Experimental Results: Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels. Animal/Disease Models: Eightweeks old (175-209 g) female rats of the Sprague- Dawley-derived strain Tif:RAlf[1] Doses: 10 and 50 mg/kg Route of Administration: Administered po (oral gavage) twice a day for 6 weeks Experimental Results: Partly prevented bone loss. |
| References |
| Molecular Formula |
C26H29N5O2.XH2O
|
|---|---|
| Related CAS # |
CGP77675;234772-64-6
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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