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Cat. No.: HY-131349

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CCR4-351

고객리뷰

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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 98.95%
CAS No.: 2174938-70-4
화학식: C₂₄H₂₇Cl₂N₇O
분자량:500.42

보관:

4°C, sealed storage, away from moisture

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

CCR4-351 Chemical Structure

CAS No.: 2174938-70-4

사이즈

가격

재고

수량

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

CCR4

All CCR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	IC₅₀	50 nM Compound: 38	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	[PMID: 32667798]
CCRF-CEM	IC₅₀	64 nM Compound: 38	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	[PMID: 32667798]

In Vitro

CCR4-351 (compound 38) shows no activity in a CYP450 induction assay^[1].
CCR4-351 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) 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 (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 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 (V_ss=5.2 L/kg), a T_1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.

Chemical Information

CAS No. 2174938-70-4
Appearance Solid
분자량 500.42
화학식 C₂₄H₂₇Cl₂N₇O
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
선적

Room temperature in continental US; may vary elsewhere.
보관

4°C, sealed storage, away from moisture

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

용액&용해도

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9983 mL

9.9916 mL

19.9832 mL

5 mM

0.3997 mL

1.9983 mL

3.9966 mL

10 mM

0.1998 mL

0.9992 mL

1.9983 mL

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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
용액&용해도
- In Vitro
순도&문서
References

상품명:
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수량:
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CCR4-351

MCE Bioactive Compound Library

All CCR Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

CCR4-351 Related Classifications

HY-131349 Related Classifications