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.
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- CAS. Nr.: 2177311-29-2
- Formel: C29H46N8O
- Molecular Weight:522.73
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
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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 |
In Vitro
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
In Vivo
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
Chemical Information
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CAS. Nr. 2177311-29-2
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Molecular Weight 522.73
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
HF51116 Related Classifications
HY-144347 Related Classifications
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