1. GPCR/G Protein Immunology/Inflammation
  2. CXCR
  3. CCX662

CCX662 is a selective CXCR7 inhibitor with human IC50 values of 9 nM (buffer) and 18 nM (100% human serum), and rat IC50 of 14 nM (100% rat serum). CCX662 blocks CXCL12 binding to CXCR7, inhibits CXCR4-directed trans-endothelial migration of CXCR4+/CXCR7+ cells. CCX662 can be used for the research of glioblastoma multiforme.

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

CCX662

CCX662 Chemical Structure

CAS No. : 1226686-54-9

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Description

CCX662 is a selective CXCR7 inhibitor with human IC50 values of 9 nM (buffer) and 18 nM (100% human serum), and rat IC50 of 14 nM (100% rat serum). CCX662 blocks CXCL12 binding to CXCR7, inhibits CXCR4-directed trans-endothelial migration of CXCR4+/CXCR7+ cells. CCX662 can be used for the research of glioblastoma multiforme[1][2].

IC50 & Target[1]

CXCR7

 

CXCL12/CXCR4

 

In Vitro

CCX662 acts as a highly potent and selective small molecule inhibitor of human and rat CXCR7 in cell-free radioligand binding assays, with IC50 values of 9 nM (buffer), 18 nM (100% human serum), and 14 nM (100% rat serum)[2].
CCX662 inhibits the CXCL12-directed trans-endothelial migration of CXCR4+/CXCR7+ NC37 cells with an IC50 of 106 nM[2].

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

In Vivo

CCX662 (0.25 mL/hr; subcutaneous infusion; 4 weeks) significantly prolongs median survival from 205 days to 370 days in rats with ENU (HY-W019815)-induced glioblastoma multiforme[1].
CXCR7 inhibition with CCX662 (subcutaneous infusion; two consecutive 7-day periods) post-irradiation significantly increases median post-irradiation survival from 6 days to 9 days in rats with intracranial C6 glioblastoma multiforme[1].
CCX662 significantly extends median survival to 234 days in the ENU-induced rat model of glioblastoma in combination with radiotherapy[2].

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

Animal Model: Sprague-Dawley (progeny of gestational day 18 dams injected with ENU; 115 days of age)[1]
Dosage: 0.25 mL/hr
Administration: subcutaneous infusion; 4 weeks
Result: Prolonged median lifespan to 370 days (compared to 205 days for irradiated vehicle-treated rats and 190 days for non-irradiated control rats).
Achieved statistically significant survival benefit (P = 0.0003, log-rank test).
Molecular Weight

539.69

Formula

C28H37N5O4S

CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

O=C(CCCOC1=C(N2CCN(CCC2)CC3=CSC(N4CCC(CC4)O)=N3)C5=NC=CC=C5C=C1C)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (185.29 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 1.8529 mL 9.2646 mL 18.5292 mL
5 mM 0.3706 mL 1.8529 mL 3.7058 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • 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

Concentration (start)

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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: ≥ 2.5 mg/mL (4.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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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).
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
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. 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 1.8529 mL 9.2646 mL 18.5292 mL 46.3229 mL
5 mM 0.3706 mL 1.8529 mL 3.7058 mL 9.2646 mL
10 mM 0.1853 mL 0.9265 mL 1.8529 mL 4.6323 mL
15 mM 0.1235 mL 0.6176 mL 1.2353 mL 3.0882 mL
20 mM 0.0926 mL 0.4632 mL 0.9265 mL 2.3161 mL
25 mM 0.0741 mL 0.3706 mL 0.7412 mL 1.8529 mL
30 mM 0.0618 mL 0.3088 mL 0.6176 mL 1.5441 mL
40 mM 0.0463 mL 0.2316 mL 0.4632 mL 1.1581 mL
50 mM 0.0371 mL 0.1853 mL 0.3706 mL 0.9265 mL
60 mM 0.0309 mL 0.1544 mL 0.3088 mL 0.7720 mL
80 mM 0.0232 mL 0.1158 mL 0.2316 mL 0.5790 mL
100 mM 0.0185 mL 0.0926 mL 0.1853 mL 0.4632 mL
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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.

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CCX662
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