Chol-CTPP
Chol-CTPP is a ligand with dual targeting effect on blood-brain barrier (BBB) and glioma cells. Lip-CTPP can be gained by Chol-CTPP and another mitochondria targeting ligand (Chol-TPP). Lip-CTPP is a promising potential carrier to exert the anti-glioma effect of doxorubicin (DOX) and lonidamine (LND) collaboratively. Lip-CTPP elevates the inhibition rate of tumor cell proliferation, migration and invasion, promote apoptosis and necrosis, and interfere with mitochondrial function.
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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。
- 分子式: C144H263N3O53
- 分子量:2884.62
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
Apoptosis, ROS[1]
Lip-CTPP shows satisfying cellular uptake and mitochondrial uptake[1].
Lip-CTPP (0-20 µg/mL DOX and LND, 24 h) shows cytotoxicity and induces apoptosis in C6 cells[1].
Lip-CTPP inhibits intracellular ATP production and has the most severe damage on the membrane potential of mitochondria[1].
Lip-CTPP possesses excellent potential to induce ROS generation[1].
Lip-CTPP (0.5 µg/mL DOX, 48 h) exhibits strong inhibitory effect both on cell migration and invasion[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C6 cells
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Concentration:0.1, 0.5, 2.5, 5, 10, and 20 µg/mL of DOX and LND
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Incubation Time:24 h
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Result:Showed cytotoxicity on C6 cells in a concentration-dependent manner.
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Cell Line:C6 cells
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Concentration:0.5 µg/mL DOX and LND
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Incubation Time:24 h
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Result:Performed excellent lethality on C6 cells and the apoptosis and necrosis rate is 3.4 times that of Free DOX + LND.
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Cell Line:C6 cells
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Concentration:0.5 µg/mL DOX
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Incubation Time:48 h
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Result:Obviously restricted the invasion of C6 cells.
Lip-CTPP can slow down the clearance of free drugs and enhance tumor targeting properties[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kunming mice (male, 20-25 g), 5 µL of C6 cells (2 × 108 cells/mL) were injected into the striatum[1]
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Dosage:3 mg/kg DOX and LND
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Administration:Tail vein injection, once on day 4, 7, 10 and 13
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Result:Increased the survival time, decreased tumor area and the density of tumor cells.
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Animal Model:Kunming mice (20-25 g)[1]
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Dosage:10 mg/kg DOX and LND
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Administration:Tail vein injection (Pharmacokinetics Analysis)
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Result:Pharmacokinetic parameters of DOX in blood after administration (mean ± SD, n = 3)[1]
parameters AUC(0-t)
(µg/mL*min)MRT (min) Tmax (min) Cmax (µg/mL) t1/2 (min) Clz (L/min/kg) Lip-CTPP 5901.90 ± 406.18 291.30 ± 1.18 30 23.31 ± 0.42 231.06 ± 43.35 1.68 ± 0.13
Pharmacokinetic parameters of DOX in brain after administration (mean ± SD, n = 3)[1]
parameters AUC(0-t)
(µg/mL*min)MRT (min) Tmax (min) Cmax (µg/mL) t1/2 (min) Clz (L/min/kg) Lip-CTPP 1757.61 ± 19.35
化学情報
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分子量 2884.62
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分子式 C144H263N3O53
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SMILES
O=C(C1=CC=C(C=C1)O)NCCOCCNC(C(CCCC2)=C2C(NCCCCCC(OCCO[C@@H](CC3)CC4=CC[C@]([C@@]5([H])[C@](CC6)([C@@](CC5)([H])[C@H](C)CCCC(C)C)C)([H])[C@@]6([H])[C@]43C)=O)=O)=O.[3].[44]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
バッチを選択:純度: 99.98%Assay: 99.98%ee.: 99.98%
参考文献
Calculators
モル濃度計算機Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)= × ×希釈計算機濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
×=× -