| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
In vitro, autophosphorylation and c-src autophosphorylation are inhibited in a dose-dependent manner with IC50 values of 1 μM and 16 μM, respectively, upon treatment with CGP52411 (DAPH; 0-100 μM; 90 min; A431 cells). Moreover, p185c-erbB2 tyrosine phosphorylation decreased concentration-dependently after CGP52411 treatment, with an IC50 value of 10 μM [1]. At an IC50 of 16 μM, CGP52411 (DAPH) inhibits c-src kinase. With an IC50 of 80 μM, CGP52411 inhibits the PKC isoenzyme that was isolated from swine brain. PKC isoenzymes that are conventional (cPKC α, β-1, β-2, and γ) are inhibited by CGP52411, while those that are atypical (aPKC η) or unconventional (nPKC δ, ε, and ζ) are not [1].
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| ln Vivo |
CGP52411 targets xenografts in vivo and shows anti-tumor action (3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, and 50 mg/kg; oral dose; daily; for 15 days; female BALB/c nude mice) [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: A431 Cell Tested Concentrations: 0 μM, 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM Incubation Duration: 90 min Experimental Results: Inhibition of autophosphorylation in a dose-dependent manner in vitro, IC50 1μM. c-src autophosphorylation is inhibited with an IC50 of 16 μM. It also resulted in a concentration-dependent decrease in tyrosine phosphorylation of p185c-erbB2, with an estimated IC50 value of 10 μM. |
| Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice injected with A431 cells [1]
Doses: 3.2 mg/kg, 6.3 mg/kg, 12.5 mg/kg, 25 mg/kg, 50 mg/kg Route of Administration: Oral; Oral; Injection Medication. Daily; continued for 15 days Experimental Results: Antitumor efficacy was obtained at doses of 50 mg/kg to 6.3 mg/kg. |
| References |
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| Additional Infomation |
4,5-dianilinophthalimide is phthalimide substituted at the 4- and 5-positions by anilino groups. It has a role as a tyrosine kinase inhibitor and a geroprotector.
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| Molecular Formula |
C₂₀H₁₅N₃O₂MOLECULARWEIGHT
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|---|---|
| Molecular Weight |
329.35
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| Exact Mass |
329.116
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| Elemental Analysis |
C, 72.94; H, 4.59; N, 12.76; O, 9.72
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| CAS # |
145915-58-8
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| PubChem CID |
1697
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| Appearance |
Yellow to orange solid powder
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| Density |
1.374 g/cm3
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| Melting Point |
199-202℃
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| LogP |
4.532
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
453
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1NC(=O)C2=CC(=C(C=C12)NC1C=CC=CC=1)NC1C=CC=CC=1
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| InChi Key |
AAALVYBICLMAMA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H15N3O2/c24-19-15-11-17(21-13-7-3-1-4-8-13)18(12-16(15)20(25)23-19)22-14-9-5-2-6-10-14/h1-12,21-22H,(H,23,24,25)
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| Chemical Name |
5,6-dianilinoisoindole-1,3-dione
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| Synonyms |
CGP52411; CGP-52411
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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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~303.63 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0363 mL | 15.1814 mL | 30.3628 mL | |
| 5 mM | 0.6073 mL | 3.0363 mL | 6.0726 mL | |
| 10 mM | 0.3036 mL | 1.5181 mL | 3.0363 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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