2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. CCR4-351

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.

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CCR4-351 Chemical Structure

CCR4-351 Chemical Structure

CAS No. : 2174938-70-4

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Based on 1 publication(s) in Google Scholar

Other Forms of CCR4-351:

CCR4-351 Related Antibodies

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • Biological Activity

  • Purity & Documentation

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Description

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[1].

IC50 & Target[1]

CCR4

 

In Vitro

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 Related Antibodies
In Vivo

CCR4-351 (compound 38; 50 mg/kg; PO; daily; for 40 days) significantly reduces the tumor growth[1].
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.

Animal Model: Six-to eight-week-old, female C57BL/6 mice with Pan02-OVA tumor[1]
Dosage: 50 mg/kg
Administration: PO; daily; for 40 days
Result: Significantly reduced the tumor growth.
Animal Model: Rat and mouse[1]
Dosage: 0.5 mg/kg of IV; 2 mg/kg of PO
Administration: IV or PO
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.
Molecular Weight

500.42

Formula

C24H27Cl2N7O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9983 mL 9.9916 mL 19.9832 mL
5 mM 0.3997 mL 1.9983 mL 3.9966 mL
View the 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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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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CCR4-351 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CCR4-3512174938-70-4CCRCC chemokine receptororallypiperidinyl-azetidinemotifantitumorCYP450Inhibitorinhibitorinhibit

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