| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| Targets |
ASK1 (IC50 = 164.1 nM); ASK2 (IC50 >20 μM)
|
|---|---|
| ln Vitro |
Attenuated cells treated with DDO3711 (15 μM; 24 hours) show anti-proliferative effects by lowering p-ASK1T838 in a PP5-dependent way. GES-1 and HGC-27 cell growth is not inhibited by DDO3711 [1]. In a concentration-dependent manner, DDO3711 (5-50 μM; 0.5-2 hours) suppresses the expression of CDK4/6 and cyclin D1 [1]. Dephosphorylation. DDO3711 lowers p-JNK and p-p38 levels in a concentration-dependent manner[1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MKN45 cells Tested Concentrations: 15 μM Incubation Duration: 24 h Experimental Results: demonstrated strong anti-proliferative activity (IC50 =0.5μM). Cell cycle analysis[1] Cell Types: MKN45 cell Tested Concentrations: 5 μM Incubation Duration: 1-24 h Experimental Results: Inhibited the expression of CDK4/6 and cyclin D1 in a concentration-dependent manner. Western Blot Analysis [1] Cell Types: MKN45 Cell Tested Concentrations: 5, 25, 50 μM Incubation Duration: 0.5-2 h Experimental Results: p-ASK1T838 can be dephosphorylated in vitro in a time- and concentration-dependent manner. |
| Animal Protocol |
Animal/Disease Models: 4weeks old BALB/c nude mice MKN45 cells [DDO3711 (20, 40 mg/kg; abdominal bladder; daily; for 21 days) Dramatically inhibited tumor growth in a dose-dependent manner [1]. 1]
Doses: 20, 40 mg/kg Route of Administration: IP; daily; continued for 21 days Experimental Results: Significant inhibition of tumor growth in a dose-dependent manner. The levels of p-ASK1T838 were Dramatically diminished. |
| References |
[1]. Qiuyue Zhang, et al. Protein Phosphatase 5-Recruiting Chimeras for Accelerating Apoptosis-Signal-Regulated Kinase 1 Dephosphorylation with Antiproliferative Activity. J Am Chem Soc. 2022 Dec 22.
|
| Molecular Formula |
C42H41N9O6
|
|---|---|
| Molecular Weight |
767.83
|
| CAS # |
2673364-10-6
|
| Related CAS # |
2673364-10-6
|
| SMILES |
C1(C(NCCCCCCNC(=O)C2=CC=C(CC3N=C(C4=CC=C(OC)C(OC)=C4)ON=3)C=C2)=O)=CC=C(C(NC2=CN3C(=N2)C=CC(N2C=NC=C2)=C3)=O)C=C1
|
| InChi Key |
JLYAXFNOILIKPP-KXQOOQHDSA-N
|
| InChi Code |
InChI=1S/C47H55ClF3N5O6S3/c1-46(2)20-18-42(34-8-12-37(48)13-9-34)36(31-46)32-55-22-24-56(25-23-55)39-14-10-35(11-15-39)45(57)53-65(60,61)41-16-17-43(44(30-41)64(58,59)47(49,50)51)52-38(19-21-54-26-28-62-29-27-54)33-63-40-6-4-3-5-7-40/h3-17,30,38,52H,18-29,31-33H2,1-2H3,(H,53,57)/t38-/m1/s1
|
| Chemical Name |
(R)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide
|
| Synonyms |
DDO3711
|
| 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 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 | 1.3024 mL | 6.5119 mL | 13.0237 mL | |
| 5 mM | 0.2605 mL | 1.3024 mL | 2.6047 mL | |
| 10 mM | 0.1302 mL | 0.6512 mL | 1.3024 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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