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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1226686-54-9
- 分子式: C28H37N5O4S
- 分子量:539.69
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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CXCR7 |
CXCL12/CXCR4 |
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.
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.
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Animal Model:Sprague-Dawley (progeny of gestational day 18 dams injected with ENU; 115 days of age)[1]
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Dosage:0.25 mL/hr
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Administration:subcutaneous infusion; 4 weeks
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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).
化学情報
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CAS 番号 1226686-54-9
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性状 Solid
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分子量 539.69
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分子式 C28H37N5O4S
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Color Yellow to orange
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SMILES
O=C(CCCOC1=C(N2CCN(CCC2)CC3=CSC(N4CCC(CC4)O)=N3)C5=NC=CC=C5C=C1C)O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
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 |