产品
编 号：F761444
分子式：C119H193N53O20S
分子量：2718.21
分子式：C119H193N53O20S
分子量：2718.21
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CAS No: 917953-08-3
产品详情
生物活性：
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells.
体内研究：
HXR9 (10 mg/kg; i.v. via the tail vein; twice weekly) blocks tumor growth.HXR9 (Initial dose of 100?mg/kg (subsequent dosing of 10?mg/kg twice weekly);Intraperitoneal; twice weekly for 18 days) blocks A549 tumour growth in vivo.Animal Model:C57black/6 mice (bearing B16 cells)
Dosage:10 mg/kg
Administration:I.v. via the tail vein; twice weekly (~30 days)
Result:Tumors showed a significant degree of growth retardation.
Animal Model:Athymic nude mice (bearing A549 cells)
Dosage:Initial dose of 100?mg/kg (subsequent dosing of 10?mg/kg twice weekly)
Administration:Intraperitoneal; twice weekly for 18 days
Result:The tumours of HXR9-treated mice were considerably smaller than those of the control groups.
体外研究：
HXR9 (60μM; 4 hours) blocks the interaction between PBX and HOX.HXR9 (60μM; 2 hours) triggersapoptosisinB16andprimarymelanoma cells.HXR9 (60μM; 2 hours) causes specific transcriptional changes.HXR9 (B16 cells) shows antiproliferative activity with an IC50 of 20μM.
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells.
体内研究：
HXR9 (10 mg/kg; i.v. via the tail vein; twice weekly) blocks tumor growth.HXR9 (Initial dose of 100?mg/kg (subsequent dosing of 10?mg/kg twice weekly);Intraperitoneal; twice weekly for 18 days) blocks A549 tumour growth in vivo.Animal Model:C57black/6 mice (bearing B16 cells)
Dosage:10 mg/kg
Administration:I.v. via the tail vein; twice weekly (~30 days)
Result:Tumors showed a significant degree of growth retardation.
Animal Model:Athymic nude mice (bearing A549 cells)
Dosage:Initial dose of 100?mg/kg (subsequent dosing of 10?mg/kg twice weekly)
Administration:Intraperitoneal; twice weekly for 18 days
Result:The tumours of HXR9-treated mice were considerably smaller than those of the control groups.
体外研究：
HXR9 (60μM; 4 hours) blocks the interaction between PBX and HOX.HXR9 (60μM; 2 hours) triggersapoptosisinB16andprimarymelanoma cells.HXR9 (60μM; 2 hours) causes specific transcriptional changes.HXR9 (B16 cells) shows antiproliferative activity with an IC50 of 20μM.
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