Cat. No.: HY-165186

Homorisedronate

Name: Homorisedronate
Brand: MedChemExpress
SKU: HY-165186
Availability: PreOrder

(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.

For research use only. We do not sell to patients.

CAS No.: 104261-69-0
Formula: C₈H₁₃NO₇P₂
Molecular Weight:297.14

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Homorisedronate Chemical Structure

CAS No.: 104261-69-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

MMP-2

40 μM (IC₅₀)

MMP-9

160 μM (IC₅₀)

MMP-12

80 μM (IC₅₀)

All MMP Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	IC50	0.64 mM	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.	S1476558610800314
ZR-75-1	IC50	0.58 mM	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.	S1476558610800314
Hs-578T	IC50	0.49 mM	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.	S1476558610800314
MCF7	IC50	0.39 mM	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.	S1476558610800314
MDA-MB-435S	IC50	0.46 mM	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.	S1476558610800314
B16-F10	IC50	0.17 mM	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.	S1476558610800314

In Vitro

OthersAnti-cancer

Others

NE-58051 (0-400 μM; 3 h) potently inhibits the proteolytic activity of purified active MMP-2, MMP-9, and MMP-12 in a dose-dependent manner, with equipotency to other tested bisphosphonates^[2].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[4]

Cell Line:

B02-GFP/βGal, MDA-MB-231, ZR-75-1, Hs578T, MCF-7, MDA-MB-435s, B16-F10
Concentration:

0.001-10 mM; IC₅₀ concentration (with or without 10 μM FOH or 10 μM GGOH)
Incubation Time:

6 days
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6J (female, 8 weeks old, 17-20 g, induced by 2-week reagent administration followed by bilateral first molar extraction)^[1]
Dosage:

250 μg/kg
Administration:

i.v.; twice weekly; 2 weeks
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.

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]
Dosage:

150 μg/kg
Administration:

s.c.; daily; 35 days
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.

Animal Model:

BALB/c (4-week-old female, subcutaneous inoculation of 5×10⁶ B02-GFP/βGal human breast cancer cells into right flank)^[4]
Dosage:

150 μg/kg
Administration:

s.c.; daily; 25 days (from day 35 to day 60 post-inoculation)
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.

Animal Model:

C57BL/6 (intravenous injection of 1×10⁶ B16-F10 melanoma cells)^[4]
Dosage:

350 μg/kg
Administration:

s.c.; daily; 14 days
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 :

Chemical Information

CAS No. 104261-69-0
Molecular Weight 297.14
Formula C₈H₁₃NO₇P₂
SMILES

O=P(O)(C(CCC1=CC=CN=C1)(P(O)(O)=O)O)O
Synonyms

NE-58051
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Kasagawa M, et al. Analysis of Risedronate Analog on Extraction Socket Healing in Mice. In vivo (Athens, Greece). 2025;39(2):648-655. [Content Brief]

[2]. Boissier S, et al. Bisphosphonates inhibit breast and prostate carcinoma cell invasion, an early event in the formation of bone metastases[J]. Cancer research, 2000, 60(11): 2949-2954.

[3]. Clézardin P, et al. Mechanisms of action of bisphosphonates in oncology: a scientific concept evolving from antiresorptive to anticancer activities. BoneKEy reports. 2013 Feb 06;2:267.

[4]. Fournier P G, et al. How do bisphosphonates inhibit bone metastasis in vivo[J]. Neoplasia, 2010, 12(7): 571-578.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Homorisedronate

All MMP Isoforms