Fenbendazole-d3 is a cadmium-labeled fenbendazole. Fenbendazole-d3 is a HIF-1α agonist that activates the HIF-1α-related GLUT1 excipient. Fenbendazole is a benzimidazole anthelmintic with adjacent activity and broad spectrum of action Fenbendazole is a microtubule stabilizer. Fenbendazole causes cell cycle and mitotic cell death and has anticancer effect in wild-type p53 xenograft mice.

Physicochemical Properties

Molecular Formula	C15H10D3N3O2S
Molecular Weight	302.366106748581
Exact Mass	302.092
CAS #	1228182-47-5
Related CAS #	Fenbendazole;43210-67-9
PubChem CID	71312505
Appearance	Off-white to light yellow solid powder
Boiling Point	209-216 °C
LogP	3.906
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	4
Heavy Atom Count	21
Complexity	363
Defined Atom Stereocenter Count	0
SMILES	COC(=O)NC1=NC2=C(N1)C=C(C=C2)SC3=CC=CC=C3
InChi Key	HDDSHPAODJUKPD-FIBGUPNXSA-N
InChi Code	InChI=1S/C15H13N3O2S/c1-20-15(19)18-14-16-12-8-7-11(9-13(12)17-14)21-10-5-3-2-4-6-10/h2-9H,1H3,(H2,16,17,18,19)/i1D3
Chemical Name	trideuteriomethyl N-(6-phenylsulfanyl-1H-benzimidazol-2-yl)carbamate
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	The inhibitory effects of miR-143-5p on proliferation, colony capacity, and migration were reversed by fenbendazole d3 (20 µM; 48 hours) [1]. In HIF-cell proliferation experiment, fenbendazole d3 (20 µM; 48 hours) improves the results [1].
Cell Assay	cell proliferation assay [1] Cell Types: BT-549 and MCF-7 cells Tested Concentrations: 20 µM Incubation Duration: 48 hrs (hours) Experimental Results: Reversal of miR-143-1α and GLUT1 protein expression levels [1]. 5p on proliferation, colony-forming ability, and migration. Western Blot Analysis[1] Cell Types: BT-549 and MCF-7 Cell Tested Concentrations: 10 µM Incubation Duration: 48 hrs (hours) Experimental Results: Increased HIF-1α and GLUT1 protein expression levels.
References	[1]. Jia Xu, et al. miR-143-5p suppresses breast cancer progression by targeting the HIF-1α-related GLUT1 pathway. Oncol Lett. 2022 May;23(5):147. [2]. Nilambra Dogra, et al. Fenbendazole acts as a moderate microtubule destabilizing agent and causes cancer cell death by modulating multiple cellular pathways. Sci Rep. 2018 Aug 9;8(1):11926. [3]. Hossein Aleyasin, et al. Antihelminthic benzimidazoles are novel HIF activators that prevent oxidative neuronal death via binding to tubulin. Antioxid Redox Signal. 2015 Jan 10;22(2):121-34. [4]. Qiwen Duan, et al. Fenbendazole as a potential anticancer drug. Anticancer Res. 2013 Feb;33(2):355-62.

Solubility Data

Solubility (In Vitro)

DMSO : ~5 mg/mL (~16.54 mM)

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.3072 mL	16.5360 mL	33.0721 mL
	5 mM	0.6614 mL	3.3072 mL	6.6144 mL
	10 mM	0.3307 mL	1.6536 mL	3.3072 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.