HF51116
HF51116 is a CXCR4 antagonist. HF51116 inhibits calcium influx/mobilization. HF51116 mobilizes HSPC and AML from bone marrow to peripheral blood in mice/monkeys, and enhances G-CSF-induced cell mobilization. HF51116 inhibits HIV-1 infection, lacks cytotoxicity in cells expressing CXCR4, and when combined with Cytarabine (HY-13605) reduces AML burden and prolongs survival in AML xenograft models.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 2177311-29-2
- 分子式: C29H46N8O
- 分子量:522.73
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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- 純度とドキュメンテーション
- 参考文献
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Calcium Channel アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
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CXCR4 |
HIV-1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
12 nM
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Inhibition of CXCR4 binding of anti-CXCR4 mAb 12G5 in CXCR4-expressing CHO cells by competitive binding assay.
Inhibition of CXCR4 binding of anti-CXCR4 mAb 12G5 in CXCR4-expressing CHO cells by competitive binding assay.
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35124530 |
| SUP-T1 | IC50 |
1.5 nM
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Inhibition of SDF-1α-induced calcium mobilization in SUP-T1 cells expressing native CXCR4.
Inhibition of SDF-1α-induced calcium mobilization in SUP-T1 cells expressing native CXCR4.
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35124530 |
体外実験
HF51116 (10-50 μM) shows no cytotoxicity in CXCR4-expressing cells[2].
HF51116 inhibits SDF-1α-induced calcium mobilization in SUP-T1 cells with an IC50 of 1.5 nM[2].
HF51116 inhibits SDF-1α-induced migration of CXCR4+ SUP-T1 cells[2].
HF51116 inhibits SDF-1α- and BMSC-induced migration of U937 and HL60 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 and B6.SJL-Ptprca Pepcb/BoyJ (CD45.2+ donor and CD45.1/CD45.2 F1 recipient; CD45.1+ recipient)[1]
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Dosage:5 mg/kg (HF51116); 100 μg/kg every 12 h for 4 days (G-CSF)
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Administration:HF51116: s.c.; once; 12 h after final G-CSF dose; G-CSF: s.c.; every 12 h; 4 days
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Result:In the G-CSF+HF51116 group, mobilization efficacy was 24,963 CFUs/mL.
The absolute number of LSK cells was 8612/mL, and the absolute number of SLAM-LSK cells was 715/mL.
Neutrophils recovered to baseline at around 18 days, and platelets recovered at around 35 days.
The percentage of CD45.2+ cells in the G-CSF+HF51116 group was 73.50% in the primary competitive transplant at 6 months.
In the secondary noncompetitive transplant at 6 months, the percentage of CD45.2+ cells was 79.11%.
- Research Protocol for Infectious Diseases
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Ca2+ Staining Technique
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
- Intraperitoneal/Peritoneal Dissemination Xenograft
化学情報
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CAS 番号 2177311-29-2
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分子量 522.73
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分子式 C29H46N8O
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SMILES
N=C(N)NCCC[C@H](NCC1=CC=CC=N1)C(NCC2=CC=C(C=C2)CNCCCNC3CCCCC3)=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
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
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
HF51116 関連分類
HY-144347 関連分類
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