CCR4-351 hydrochloride

Name: CCR4-351 hydrochloride
Brand: MedChemExpress
SKU: HY-131349A
Rating: 4.5 (1 reviews)

Cat. No.: HY-131349A Purity: 98.37%: FAQs
Data Sheet SDS COA Handling Instructions

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CCR4-351 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4-351 hydrochloride, featuring a novel piperidinyl-azetidine motif, has IC₅₀s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 hydrochloride has antitumor activity.

For research use only. We do not sell to patients.

CCR4-351 hydrochloride Chemical Structure

CAS No. : 2174938-71-5

Size	Price	Stock	Quantity
1 mg	USD 523	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 1150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1800	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 3600	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 5750	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 9200	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of CCR4-351 hydrochloride:

CCR4-351 Get quote

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•Related Small Molecules:

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View All Isoforms

CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

CCR4

In Vitro

CCR4-351 (compound 38) hydrochloride shows no activity in a CYP450 induction assay^[1].
CCR4-351 hydrochloride inhibits the migration of mouse iT_reg cells with an IC₅₀ of 39 nM, while the IC₅₀ in human iT_reg cells is 33 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CCR4-351 (compound 38; 50 mg/kg; PO; daily; for 40 days) hydrochloride significantly reduces the tumor growth^[1].
CCR4-351 (0.5 mg/kg; IV) hydrochloride has low clearance (CL=10.2 mL/min/kg), medium volume of distribution (V_ss=5.2 L/kg), a T_1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse^[1].
CCR4-351 hydrochloride has low clearance (CL=7.3 mL/min/kg), a half-life of 12.7 hr, and is 44% bioavailable in dog. CCR4-351 hydrochloride 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 (V_ss=5.2 L/kg), a T_1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.

Formula

C₂₄H₂₈Cl₃N₇O

CAS No.

2174938-71-5

Appearance

Solid

Color

White to off-white

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.[H]Cl.[x]

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 : 170 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 4.25 mg/mL; Clear solution

This protocol yields a clear solution of ≥ 4.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (42.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 4.25 mg/mL; Clear solution

This protocol yields a clear solution of ≥ 4.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (42.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.37%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (253 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

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. [Content Brief]