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Chemical Structure| 165800-06-6 Chemical Structure| 165800-06-6

Structure of Zoledronic acid monohydrate
CAS No.: 165800-06-6

Chemical Structure| 165800-06-6

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Zoledronic acid is an activator of protein kinase C with apoptotic effects on multiple myeloma cell lines.

Synonyms: Zoledronate monohydrate; CGP42446A monohydrate; Zoledronic Acid(hydrate)

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Product Details of Zoledronic acid monohydrate

CAS No. :165800-06-6
Formula : C5H12N2O8P2
M.W : 290.10
SMILES Code : OC(P(O)(O)=O)(P(O)(O)=O)CN1C=CN=C1.[H]O[H]
Synonyms :
Zoledronate monohydrate; CGP42446A monohydrate; Zoledronic Acid(hydrate)
MDL No. :MFCD08448695
InChI Key :FUXFIVRTGHOMSO-UHFFFAOYSA-N
Pubchem ID :121586

Safety of Zoledronic acid monohydrate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H361
Precautionary Statements:P501-P202-P201-P264-P280-P302+P352-P308+P313-P337+P313-P305+P351+P338-P362+P364-P332+P313-P405

Related Pathways of Zoledronic acid monohydrate

epigenetics
GPCR

Isoform Comparison

Biological Activity

Description
Zoledronic acid monohydrate (Zoledronate monohydrate) is a third-generation bisphosphonate (BP) with potent anti-resorptive activity. It inhibits the differentiation and apoptosis of osteoclasts and also exhibits anti-cancer effects [1].

In Vitro:

Cell Line
Concentration Treated Time Description References
γδ T cells 3 μg/mL 5 days Activate γδ T cells for subsequent experiments Nat Commun. 2021 Feb 4;12(1):792.
U-2OS cells 1 µM 24 h To investigate the effect of Zoledronic acid on Ras/Akt/mTOR and Ras/ERK1/2/HIF-1α signaling pathways, it was found to inhibit these pathways, increase ABCA1 expression, and restore immune sensitivity. Cells. 2020 Mar 6;9(3):647.
Saos-2 cells 1 µM 24 h To investigate the effect of Zoledronic acid on Saos-2 cells, it was found to increase ABCA1 expression and restore immune sensitivity. Cells. 2020 Mar 6;9(3):647.
leukemia cells 1 μM or 10 μM 48 h To evaluate the effect of Zoledronic acid on the viability of leukemia cells, results showed that Zoledronic acid had no direct effect on the viability and colony-forming capacity of leukemia cells. Leukemia. 2018 Nov;32(11):2326-2338.
γδ T cells 2 μM 24 h To expand γδ T cells, results showed that zoledronic acid effectively promoted the expansion of γδ T cells. MAbs. 2022 Jan-Dec;14(1):2115205.
Cervical cancer cells derived CSCs 5, 10, 20, 40, 80 μM 1, 2, 3, 4, 5 days Zoledronic acid inhibited the proliferation of cervical cancer cells derived CSCs, with an IC50 of 23.39 μM at 72 h J Exp Clin Cancer Res. 2019 Feb 21;38(1):93.
HeLa cells derived CSCs 10, 20, 30 μM 72 h Zoledronic acid induced apoptosis in HeLa cells derived CSCs, with the apoptotic proportion increasing from 3.2% to 36.2% J Exp Clin Cancer Res. 2019 Feb 21;38(1):93.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice B16-F10 tumor model Intraperitoneal injection 5 mg/kg Every 4 days for a total of 5 times To reduce the population of tumor-associated macrophages (TAMs), thereby decreasing the accumulation of DOX-AS-M-NPs in tumors Mol Pharm. 2014 Dec 1;11(12):4425-36
BALB/c nude mice Bone metastasis model Intraperitoneal injection 100 μg/kg On days 1, 3 and 7 Zoledronic acid combined with PTX and 4D3 enhanced the antitumor effect, significantly inhibiting tumor growth. Cancer Sci. 2020 May;111(5):1840-1850
Mice Hu-CD34+ mouse model Intravenous injection 20 µg/mice Administered on days 3, 9, and 15, lasting 21 days To investigate the therapeutic effect of Zoledronic acid on chemo-immune-resistant osteosarcoma, it was found to slow tumor growth, increase intratumor necrosis and apoptosis, and enhance the ABCA1/ABCB1 ratio and Vγ9Vδ2 T-cell infiltration. Cells. 2020 Mar 6;9(3):647.
Mice Osteoporosis model Intraperitoneal injection 0.25 mg/kg Twice a week for 2 weeks ZA prevented CLP-induced bone loss Sci Rep. 2017 Feb 1;7:41358
Mice Sfrp4 knockout mice Intraperitoneal injection 20 µg/kg Single dose, male mice observed up to 68 weeks, female mice observed up to 24 weeks Zoledronic acid treatment does not interfere with the development of elevated trabecular bone mass with Sfrp4 disruption and does not differentially affect cortical bone width or thickness. Bone Res. 2023 Feb 20;11(1):9
Mice BCR-ABL1+ pre-B ALL model Intraperitoneal injection 2 μg 5 days a week for 2 weeks To evaluate the therapeutic effect of Zoledronic acid on leukemia-induced bone loss, results showed that Zoledronic acid inhibited the activity of osteoclasts, restored the bone loss, reduced the bone resorption activity, and prolonged the survival of mice. Leukemia. 2018 Nov;32(11):2326-2338.
BALB/c nude mice Xenograft model of cervical cancer cells derived CSCs Intraperitoneal injection 20, 40, 80 μg/kg Once daily for 21 days Zoledronic acid suppressed the growth of xenografts derived from HeLa cells derived CSCs, significantly reducing tumor volume and weight J Exp Clin Cancer Res. 2019 Feb 21;38(1):93.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.45mL

0.69mL

0.34mL

17.23mL

3.45mL

1.72mL

34.47mL

6.89mL

3.45mL

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