CCR4-351
Based on 1 Customer Validation
CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity.
For research use only. We do not sell to patients.
- Purity: 98.95%
- CAS No.: 2174938-70-4
- Formula: C24H27Cl2N7O
- Molecular Weight:500.42
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CCR4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | IC50 |
50 nM
Compound: 38
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Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
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[PMID: 32667798] |
| CCRF-CEM | IC50 |
64 nM
Compound: 38
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Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL17-mediated chemotaxis preincubated for 30 mins followed by CCL17 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL17-mediated chemotaxis preincubated for 30 mins followed by CCL17 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
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[PMID: 32667798] |
CCR4-351 (compound 38) shows no activity in a CYP450 induction assay[1].
CCR4-351 inhibits the migration of mouse iTreg cells with an IC50 of 39 nM, while the IC50 in human iTreg cells is 33 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CCR4-351 (0.5 mg/kg; IV) has low clearance (CL=10.2 mL/min/kg), medium volume of distribution (Vss=5.2 L/kg), a T1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse[1].
CCR4-351 has low clearance (CL=7.3 mL/min/kg), a half-life of 12.7 hr, and is 44% bioavailable in dog. CCR4-351 has low clearance (CL=3.7 mL/min/kg), a long terminal half-life (10.7 hr), and good bioavailability (%F = 41) in cynomolgus monkey[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-to eight-week-old, female C57BL/6 mice with Pan02-OVA tumor[1]
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Dosage:50 mg/kg
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Administration:PO; daily; for 40 days
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Result:Significantly reduced the tumor growth.
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Animal Model:Rat and mouse[1]
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Dosage:0.5 mg/kg of IV; 2 mg/kg of PO
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Administration:IV or PO
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Result:Possessed medium clearance (CL=47.6 mL/min/kg) and was 49% bioavailable upon oral dosing in rat.
Had low clearance (CL=10.2 mL/min/kg), medium volume of distribution (Vss=5.2 L/kg), a T1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.
Chemical Information
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CAS No. 2174938-70-4
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Appearance Solid
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Molecular Weight 500.42
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Formula C24H27Cl2N7O
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Color Light yellow to yellow
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SMILES
[H][C@@]1(CCCN(C1)CCO)C2CN(C2)C3=CN=C(C4=N3)C(C#N)=NN4[C@H](C)C5=CC=C(C=C5Cl)Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 190 mg/mL (379.68 mM; Need ultrasonic; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Purity & Documentation
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Data Sheet (275 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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Handling Instructions (2659 KB)
References
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 (sealed storage, away from moisture). 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 | 1.9983 mL | 9.9916 mL | 19.9832 mL | 49.9580 mL |
| 5 mM | 0.3997 mL | 1.9983 mL | 3.9966 mL | 9.9916 mL | |
| 10 mM | 0.1998 mL | 0.9992 mL | 1.9983 mL | 4.9958 mL | |
| 15 mM | 0.1332 mL | 0.6661 mL | 1.3322 mL | 3.3305 mL | |
| 20 mM | 0.0999 mL | 0.4996 mL | 0.9992 mL | 2.4979 mL | |
| 25 mM | 0.0799 mL | 0.3997 mL | 0.7993 mL | 1.9983 mL | |
| 30 mM | 0.0666 mL | 0.3331 mL | 0.6661 mL | 1.6653 mL | |
| 40 mM | 0.0500 mL | 0.2498 mL | 0.4996 mL | 1.2490 mL | |
| 50 mM | 0.0400 mL | 0.1998 mL | 0.3997 mL | 0.9992 mL | |
| 60 mM | 0.0333 mL | 0.1665 mL | 0.3331 mL | 0.8326 mL | |
| 80 mM | 0.0250 mL | 0.1249 mL | 0.2498 mL | 0.6245 mL | |
| 100 mM | 0.0200 mL | 0.0999 mL | 0.1998 mL | 0.4996 mL |
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