OTX008 (Synonyms: Calixarene 0118, PTX008) |
Catalog No.GC18756
One-Click Copy Product Info
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OTX008 is a selective inhibitor of galectin-1.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 286936-40-1
Sample solution is provided at 25 µL, 10mM.
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OTX008 is a selective inhibitor of galectin-1 [1]. OTX008 specifically binds to the β-pleated folded domain of Gal-1, inducing oxidation and proteasomal degradation, thereby inhibiting tumor cell proliferation, invasion, and angiogenesis [2]. OTX008 is indicated for the treatment of various solid tumors [3-4].
In ARPE-19 cells, OTX008 (2.5-10µM; 4h) treatment significantly increased cell viability in high glucose [5]. In OSSC cells, OTX008 (12.5-100μg/mL; 24-72h) reduces cell viability in a dose-dependent manner [6].
In SQ20B cells xenograft mice model, OTX008 (10mg/kg; ip; 21d) inhibits tumor growth [7]. In 293FT cells xenograft mice model, OTX008 (3mg/kg; ip; 3d) inhibits tumor growth [8].
References:
[1]. Astorgues-Xerri L, Riveiro M E, Tijeras-Raballand A, et al. OTX008, a selective small-molecule inhibitor of galectin-1, downregulates cancer cell proliferation, invasion and tumour angiogenesis[J]. European journal of cancer, 2014, 50(14): 2463-2477.
[2]. Delord J P, Awada A, Raymond E, et al. Abstract A72: A first-in-man Phase I study of the galectin-1 (gal-1) inhibitor OTX008 given subcutaneously as a single agent to patients with advanced solid tumors[J]. Molecular Cancer Therapeutics, 2013, 12(11_Supplement): A72-A72.
[3]. Zucchetti M, Bonezzi K, Frapolli R, et al. Pharmacokinetics and antineoplastic activity of galectin-1-targeting OTX008 in combination with sunitinib[J]. Cancer chemotherapy and pharmacology, 2013, 72(4): 879-887.
[4]. Rezai K, Durand S, Lachaux N, et al. OTX008 pharmacokinetics (PK) during the first-in-man phase I study in patients with advanced solid tumors[J]. Cancer Research, 2013, 73(8_Supplement): 33-33.
[5]. Trotta M C, Petrillo F, Gesualdo C, et al. Effects of the Calix [4] arene derivative compound OTX008 on high glucose-stimulated ARPE-19 cells: Focus on galectin-1/TGF-β/EMT pathway[J]. Molecules, 2022, 27(15): 4785.
[6]. Greer P. Effects of OTX008, a galectin-1 inhibitor, on oral squamous cell carcinoma cells in vitro[D]. University of Otago, 2018.
[7]. Koonce N A, Griffin R J, Dings R P M. Galectin-1 inhibitor OTX008 induces tumor vessel normalization and tumor growth inhibition in human head and neck squamous cell carcinoma models[J]. International journal of molecular sciences, 2017, 18(12): 2671.
[8]. Leung Z, Ko F C F, Tey S K, et al. Galectin-1 promotes hepatocellular carcinoma and the combined therapeutic effect of OTX008 galectin-1 inhibitor and sorafenib in tumor cells[J]. Journal of Experimental & Clinical Cancer Research, 2019, 38(1): 423.
| Cell experiment [1]: | |
Cell lines | ARPE-19 cells |
Preparation Method | Human ARPE-19 cells were cultured in Dulbecco's Modified Eagle Medium/Nutrient Mixture F12 (DMEM/F12) at 37℃ and 5% CO2 with 5mM glucose. The culture medium was supplemented with 10% heat-inactivated fetal bovine serum (FBS), 1% penicillin/streptomycin solution (P/S), 1% L-glutamine (L-Glu), 5mM Hepes, and 7.5% NaHCO3. Two days after plating, cells were split and seeded into separate culture dishes at varying cell densities for each experiment. For the first three days, cells were exposed to 5mM D-glucose (normal glucose, NG); 35mM D-glucose (high glucose, HG); and 5mM D-glucose and 30mM mannitol (NG+M) (as a negative control for high glucose) at 37℃ and 5% CO2. Then, after 72h of NG or HG stimulation, OTX008 was dissolved in 0.1% w/v dimethyl sulfoxide (DMSO) as a vehicle or 0.1% DMSO in fresh cell culture medium (NG or HG) and added daily until day 9. |
Reaction Conditions | 2.5-10µM; 4h |
Applications | OTX008 treatment significantly increased cell viability in high glucose. |
| Animal experiment [2]: | |
Animal models | SQ20B cells xenograft mice model |
Preparation Method | For the xenograft model, female athymic nude mice (Nu/Nu, 5-6 weeks old) were inoculated subcutaneously with tumor cells into the right abdominal cavity. When tumors reached approximately 100 cubic millimeters, animals were randomly assigned to treatment groups and began receiving OTX008. A total of 92 animals were inoculated, and 76 tumor-bearing animals were randomized before the start of intervention. |
Dosage form | 10mg/kg; ip; 21d |
Applications | OTX008 inhibits tumor growth. |
References: | |
| Cas No. | 286936-40-1 | SDF | |
| Synonyms | Calixarene 0118, PTX008 | ||
| Chemical Name | 2,2',2'',2'''-[pentacyclo[19.3.1.13,7.19,13.115,19]octacosa-1(25),3,5,7(28),9,11,13(27),15,17,19(26),21,23-dodecaene-25,26,27,28-tetrayltetrakis(oxy)]tetrakis[N-[2-(dimethylamino)ethyl]-acetamide | ||
| Canonical SMILES | O=C(NCCN(C)C)COC1=C(C2)C=CC=C1CC3=CC=CC(CC4=CC=CC(CC5=CC=CC2=C5OCC(NCCN(C)C)=O)=C4OCC(NCCN(C)C)=O)=C3OCC(NCCN(C)C)=O | ||
| Formula | C52H72N8O8 | M.Wt | 937.2 |
| Solubility | DMF: 1 mg/ml,DMSO: 2 mg/ml,Ethanol: 5 mg/ml,PBS (pH 7.2): 0.5 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.067 mL | 5.335 mL | 10.6701 mL |
| 5 mM | 213.4 μL | 1.067 mL | 2.134 mL |
| 10 mM | 106.7 μL | 533.5 μL | 1.067 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)