GLPBio

OTX008

Catalog No.: GC18756Purity:>98.00%Synonyms: Calixarene 0118, PTX008
COASDSData Sheet
OTX008 is a selective inhibitor of galectin-1.

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OTX008
Cas No.: 286936-40-1
10mM (in 1mL DMSO)In Stock
$183.00
1
1mgIn Stock
$60.00
1
5mgIn Stock
$116.00
1
10mgIn Stock
$177.00
1
25mgIn Stock
$301.00
1
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Description

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.

Protocol

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:
[1]. 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-?/EMT pathway[J]. Molecules, 2022, 27(15): 4785.
[2]. 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.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
286936-40-1
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
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
Molecular Formula
C52H72N8O8
Molecular Weight
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
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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