Homorisedronate
(Synonyms: NE-58051)
Homorisedronate (NE-58051) is a MMP inhibitor with high bone mineral affinity but low bone antiresorptive activity in vivo. Homorisedronate inhibits the proteolytic activity of MMP-2, MMP-9, and MMP-12 through zinc chelation and phosphonate groups, with IC50 values of 40 μM, 160 μM, and 80 μM for human MMP-2, mouse MMP-9, and rabbit MMP-12, respectively. Homorisedronate inhibits breast cancer and melanoma cell proliferation without inducing MRONJ-like lesions, altering osteoclast activity, or changing serum TRAcP-5b levels. Homorisedronate is suitable for research related to breast cancer and melanoma.
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- CAS No.: 104261-69-0
- 화학식: C8H13NO7P2
- 분자량:297.14
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- 순도&문서
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Biological Activity
제품 설명
Homorisedronate (NE-58051) is a MMP inhibitor with high bone mineral affinity but low bone antiresorptive activity in vivo. Homorisedronate inhibits the proteolytic activity of MMP-2, MMP-9, and MMP-12 through zinc chelation and phosphonate groups, with IC50 values of 40 μM, 160 μM, and 80 μM for human MMP-2, mouse MMP-9, and rabbit MMP-12, respectively. Homorisedronate inhibits breast cancer and melanoma cell proliferation without inducing MRONJ-like lesions, altering osteoclast activity, or changing serum TRAcP-5b levels. Homorisedronate is suitable for research related to breast cancer and melanoma[1][2][3][4].
IC50 & Target
[1]|
MMP-2 40 μM (IC50) |
MMP-9 160 μM (IC50) |
MMP-12 80 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
0.64 mM
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Antiproliferative activity against human breast cancer MDA-MB-231 cells assessed as reduction in cell viability incubated for 6 days by MTT assay.
Antiproliferative activity against human breast cancer MDA-MB-231 cells assessed as reduction in cell viability incubated for 6 days by MTT assay.
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S1476558610800314 |
| ZR-75-1 | IC50 |
0.58 mM
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Antiproliferative activity against human breast cancer ZR-75-1 cells assessed as reduction in cell viability incubated for 6 days by MTT assay.
Antiproliferative activity against human breast cancer ZR-75-1 cells assessed as reduction in cell viability incubated for 6 days by MTT assay.
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S1476558610800314 |
| Hs-578T | IC50 |
0.49 mM
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Antiproliferative activity against human breast cancer Hs578T cells assessed as reduction in cell viability incubated for 6 days by MTT assay.
Antiproliferative activity against human breast cancer Hs578T cells assessed as reduction in cell viability incubated for 6 days by MTT assay.
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S1476558610800314 |
| MCF7 | IC50 |
0.39 mM
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Antiproliferative activity against human breast cancer MCF-7 cells assessed as reduction in cell viability incubated for 6 days by MTT assay.
Antiproliferative activity against human breast cancer MCF-7 cells assessed as reduction in cell viability incubated for 6 days by MTT assay.
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S1476558610800314 |
| MDA-MB-435S | IC50 |
0.46 mM
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Antiproliferative activity against human breast cancer MDA-MB-435s cells assessed as reduction in cell viability incubated for 6 days by MTT assay.
Antiproliferative activity against human breast cancer MDA-MB-435s cells assessed as reduction in cell viability incubated for 6 days by MTT assay.
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S1476558610800314 |
| B16-F10 | IC50 |
0.17 mM
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Antiproliferative activity against mouse melanoma B16-F10 cells assessed as reduction in cell viability incubated for 6 days by MTT assay.
Antiproliferative activity against mouse melanoma B16-F10 cells assessed as reduction in cell viability incubated for 6 days by MTT assay.
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S1476558610800314 |
In Vitro
OthersAnti-cancer
Others
Anti-cancer
Homorisedronate (NE-58051) inhibits proliferation of breast cancer cells in vitro[3].
Homorisedronate (0.001-10 mM; 6 days) dose-dependently inhibits proliferation of B02-GFP/βGal, MDA-MB-231, ZR-75-1, Hs578T, MCF-7, MDA-MB-435s, and B16-F10 cells in vitro with IC50 values ranging from 0.17 mM to 0.64 mM, via a mechanism independent of the mevalonate pathway downstream of farnesyl pyrophosphate synthase[4].
Homorisedronate (0.001-10 mM; 6 days) dose-dependently inhibits proliferation of B02-GFP/βGal, MDA-MB-231, ZR-75-1, Hs578T, MCF-7, MDA-MB-435s, and B16-F10 cells in vitro with IC50 values ranging from 0.17 mM to 0.64 mM, via a mechanism independent of the mevalonate pathway downstream of farnesyl pyrophosphate synthase[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[4]
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Cell Line:B02-GFP/βGal, MDA-MB-231, ZR-75-1, Hs578T, MCF-7, MDA-MB-435s, B16-F10
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Concentration:0.001-10 mM; IC50 concentration (with or without 10 μM FOH or 10 μM GGOH)
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Incubation Time:6 days
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Result:Induced dose-dependent inhibition of proliferation in all tested cell lines.
Exhibited IC50 values of 0.61 mM (B02-GFP/βGal), 0.64 mM (MDA-MB-231), 0.58 mM (ZR-75-1), 0.49 mM (Hs578T), 0.39 mM (MCF-7), 0.46 mM (MDA-MB-435s), and 0.17 mM (B16-F10).
Failed to have its proliferation inhibition effect on B02-GFP/βGal cells reversed by cotreatment with FOH or GGOH.
In Vivo
OthersAnti-cancer
Others
Homorisedronate (250 μg/kg; i.v.; twice weekly; 2 weeks) does not induce MRONJ-like lesions in female C57BL/6J mice, as evidenced by empty osteocytic lacunae and necrotic bone area values comparable to saline-treated controls[1].
Anti-cancer
Homorisedronate (150 μg/kg; s.c.; daily; 35 days) does not inhibit breast cancer bone metastasis formation, reduce skeletal tumor burden, or decrease osteolytic lesion area in BALB/c athymic mice[4].
Homorisedronate (150 μg/kg; s.c.; daily; 25 days) does not inhibit growth of subcutaneous breast cancer xenografts in BALB/c mice[4].
Homorisedronate (350 μg/kg; s.c.; daily; 14 days) does not inhibit melanoma lung metastasis formation in C57BL/6 mice[4].
Homorisedronate (150 μg/kg; s.c.; daily; 25 days) does not inhibit growth of subcutaneous breast cancer xenografts in BALB/c mice[4].
Homorisedronate (350 μg/kg; s.c.; daily; 14 days) does not inhibit melanoma lung metastasis formation in C57BL/6 mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (female, 8 weeks old, 17-20 g, induced by 2-week reagent administration followed by bilateral first molar extraction)[1]
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Dosage:250 μg/kg
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Administration:i.v.; twice weekly; 2 weeks
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Result:Showed complete mucosal closure of tooth extraction sockets, similar to control mice.
Revealed new bone formation within extraction sockets, with empty osteocytic lacunae counts and necrotic bone area percentages matching those of saline-treated control mice.
Showed no significant differences in total TRAP-positive cell counts, bone surface-adhered TRAP-positive cell counts, detached TRAP-positive cell counts, or serum TRAcP-5b levels relative to controls.
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Animal Model:BALB/c athymic (nu/nu) (4-week-old female, intravenous injection of 5×105 B02-GFP/βGal human breast cancer cells via tail vein)[4]
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Dosage:150 μg/kg
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Administration:s.c.; daily; 35 days
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Result:Produced mean osteolytic lesion area of 5.0 mm2.
Produced bone volume-to-tissue volume (BV/TV) ratio of 15.0%.
Produced mean tumor burden area of 20.4 mm2.
Produced tumor burden-to-soft tissue volume (TB/STV) ratio of 16.5%.
Maintained bone marrow CTX-I levels similar to vehicle-treated controls.
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Animal Model:BALB/c (4-week-old female, subcutaneous inoculation of 5×106 B02-GFP/βGal human breast cancer cells into right flank)[4]
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Dosage:150 μg/kg
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Administration:s.c.; daily; 25 days (from day 35 to day 60 post-inoculation)
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Result:Failed to inhibit growth of subcutaneous B02-GFP/βGal tumor xenografts.
Resulted in tumor volume comparable to vehicle-treated controls at all measured time points.
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Animal Model:C57BL/6 (intravenous injection of 1×106 B16-F10 melanoma cells)[4]
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Dosage:350 μg/kg
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Administration:s.c.; daily; 14 days
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Result:Failed to inhibit formation of B16-F10 melanoma lung metastases.
Resulted in number of visible pigmented lung metastases comparable to vehicle-treated controls.
Related Protocols :
- Mitochondrial membrane-potential fluorescent assay
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Mitochondrial membrane-potential and mitochondrial mass staining
- MTT Cell Proliferation Assay
- Osteoclast differentiation from monocyte/macrophage precursors
Chemical Information
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CAS No. 104261-69-0
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분자량 297.14
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화학식 C8H13NO7P2
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SMILES
O=P(O)(C(CCC1=CC=CN=C1)(P(O)(O)=O)O)O
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Synonyms
NE-58051
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
Select Batch:
Purity:
99.98%
Assay:
99.98%
ee.:
99.98%
References
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Homorisedronate Related Classifications
HY-165186 Related Classifications
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