| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
P2X2/3[2]
Minodronic acid targets the mevalonate pathway, specifically inhibiting geranylgeranyl pyrophosphate (GGPP) biosynthesis. This inhibition disrupts signal transduction in the Ras-mitogen-activated protein kinase pathway, thereby inhibiting RANKL expression on bone marrow stromal cells. By inhibiting RANKL expression, minodronic acid suppresses bone resorption mediated by osteoclasts. The compound also directly affects cancer cells by inducing apoptosis and inhibiting proliferation. |
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| ln Vitro |
Minodronic acid demonstrates potent in vitro activity against various cancer cell lines. It directly and indirectly prevents proliferation, induces apoptosis, and inhibits metastasis of various types of cancer cells. In a study on bladder cancer, minodronic acid successfully prevented the growth of cancer cells in vitro. The compound's ability to inhibit RANKL expression in bone marrow stromal cell lines has also been demonstrated.
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| ln Vivo |
In vivo activity of minodronic acid has been demonstrated in several animal models. It prevented arthritis by suppressing bone resorption in rats with collagen-induced arthritis. The compound successfully prevented the growth of bladder cancer in vivo. It may suppress arthritis by inhibiting the increase in inflammatory cytokine levels.
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| Enzyme Assay |
In vitro enzyme assays for minodronic acid involve measuring its inhibition of GGPP biosynthesis in the mevalonate pathway. The compound's effects on RANKL expression can be assessed using bone marrow stromal cell lines, where RANKL mRNA and protein levels are measured following treatment. The inhibition of the Ras-MAPK signaling pathway can be evaluated by Western blotting for phosphorylated proteins.
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| Cell Assay |
In vitro cellular assays for minodronic acid involve treating cancer cell lines (such as bladder cancer cells) with varying concentrations of the compound. Cell proliferation is assessed using MTT or other viability assays. Apoptosis is evaluated by Annexin V staining, caspase activity assays, or DNA fragmentation analysis. RANKL expression can be measured in bone marrow stromal cells using qRT-PCR or ELISA.
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| Animal Protocol |
In vivo animal experiments for minodronic acid have been conducted in rat models of collagen-induced arthritis, where the compound is administered and efficacy is evaluated by measuring bone resorption and arthritis severity. The compound has also been evaluated in mouse models of bladder cancer, where tumor growth inhibition is assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for minodronic acid are limited. As a third-generation bisphosphonate, it has a heterocyclic R2 side chain that contributes to its 100-fold greater potency compared to other bisphosphonates. The compound is typically administered orally or parenterally. Its absorption, distribution, metabolism, and excretion properties are characteristic of bisphosphonates, which have a strong affinity for bone tissue.
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| Toxicity/Toxicokinetics |
Toxicological data for minodronic acid are consistent with those of other bisphosphonates. Nitrogen-containing bisphosphonates can cause gastrointestinal irritation, hypocalcemia, and renal toxicity at high doses. The compound should be handled with appropriate safety precautions in research settings. It is intended for research use only.
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| References |
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| Additional Infomation |
See also: Minodronic acid monohydrate (note moved to).
Drug indications Studied for the treatment of multiple myeloma, breast cancer, osteoporosis, and lung cancer. Minodronic acid (YM-529) (CAS#: 180064-38-4) has the molecular formula C9H12N2O7P2·H2O and a molecular weight of 340.16 (anhydrous). It is a third-generation nitrogen-containing bisphosphonate that inhibits GGPP biosynthesis in the mevalonate pathway and subsequently signal transduction in the Ras-MAPK pathway, thereby inhibiting RANKL expression. The compound has shown direct anticancer effects. |
| Molecular Formula |
C9H12N2O7P2
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|---|---|
| Molecular Weight |
322.15
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| Exact Mass |
322.012
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| CAS # |
180064-38-4
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| Related CAS # |
Minodronic acid-d4;1807367-80-1
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| PubChem CID |
130956
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| Appearance |
White to off-white solid powder
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| Density |
1.973 g/cm3
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| LogP |
-2.2
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
439
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VMMKGHQPQIEGSQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H12N2O7P2/c12-9(19(13,14)15,20(16,17)18)5-7-6-10-8-3-1-2-4-11(7)8/h1-4,6,12H,5H2,(H2,13,14,15)(H2,16,17,18)
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| Chemical Name |
(1-hydroxy-2-imidazo[1,2-a]pyridin-3-yl-1-phosphonoethyl)phosphonic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : 5 mg/mL (15.52 mM )
DMSO : < 1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (6.21 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1041 mL | 15.5207 mL | 31.0414 mL | |
| 5 mM | 0.6208 mL | 3.1041 mL | 6.2083 mL | |
| 10 mM | 0.3104 mL | 1.5521 mL | 3.1041 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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