| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
CCR4-351 (compound 38) had little activity in CYP450 induction tests [1]. The IC50 of CCR4-351 is 39 nM for mouse iTreg cells and 33 nM for human iTreg cells, respectively, to inhibit their migration [1].
|
|---|---|
| ln Vivo |
CCR4-351 (Compound 38; 50 mg/kg; oral; daily; for 40 days) effectively suppresses tumor development [1]. CCR4-351 (0.5 mg/kg; IV) had low clearance (CL=10.2 mL/min/kg), medium volume of distribution (Vss=5.2 L/kg), T1/2 of 6.9 h, and good bioavailability (%F = 29) Orally given to mice [1]. CCR4-351 has a low clearance (CL=7.3 mL/min/kg), a half-life of 12.7 hours, and a bioavailability of 44% in dogs. CCR4-351 has low clearance (CL=3.7 mL/min/kg), extended terminal half-life (10.7 hours), and good bioavailability (%F = 41) in cynomolgus monkeys [1].
|
| Animal Protocol |
Animal/Disease Models: 6 to 8 weeks old female C57BL/6 mice with Pan02-OVA tumors [1]
Doses: 50 mg/kg Route of Administration: Oral; daily; continued for 40 days Experimental Results: Significant reduction in tumor growth . Animal/Disease Models: Rat and Mouse[1] Doses: 0.5 mg/kg IV; 2 mg/kg PO Route of Administration: IV or PO Experimental Results: Rats had moderate clearance after oral administration (CL=47.6 mL/min /kg) and the bioavailability is 49%. Oral administration to mice demonstrated low clearance (CL=10.2 mL/min/kg), medium volume of distribution (Vss=5.2 L/kg), T1/2 of 6.9 hrs (hrs (hours)), and good bioavailability (%F = 29) . |
| References |
[1]. Omar Robles, et al. Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as Single Agent and in Combination with Checkpoint Inhibitors. J Med Chem. 2020 Jul 15.
|
| Molecular Formula |
C24H27CL2N7O
|
|---|---|
| Molecular Weight |
500.428
|
| CAS # |
2174938-70-4
|
| Related CAS # |
CCR4-351 hydrochloride;2174938-71-5
|
| SMILES |
C12N([C@@H](C3=CC=C(Cl)C=C3Cl)C)N=C(C#N)C1=NC=C(N1CC([C@H]3CCCN(CCO)C3)C1)N=2
|
| 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) |
DMSO : ~190 mg/mL (~379.68 mM)
|
|---|---|
| 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 | 1.9983 mL | 9.9914 mL | 19.9828 mL | |
| 5 mM | 0.3997 mL | 1.9983 mL | 3.9966 mL | |
| 10 mM | 0.1998 mL | 0.9991 mL | 1.9983 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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