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Chemical Structure| 286936-40-1 Chemical Structure| 286936-40-1

Structure of OTX008
CAS No.: 286936-40-1

Chemical Structure| 286936-40-1

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OTX008 is a calixarene-based compound and selective galectin-1 (Gal-1) inhibitor with potential anti-angiogenic and antineoplastic activities.

Synonyms: Calixarene 0118; PTX008; N(2dimethylamino)ethyl)acetamidyl calix4arene.

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Product Details of OTX008

CAS No. :286936-40-1
Formula : C52H72N8O8
M.W : 937.18
SMILES Code : O=C(NCCN(C)C)COC1=C(CC2=C(OCC(NCCN(C)C)=O)C(C3)=CC=C2)C=CC=C1CC4=C(OCC(NCCN(C)C)=O)C(CC5=CC=CC3=C5OCC(NCCN(C)C)=O)=CC=C4
Synonyms :
Calixarene 0118; PTX008; N(2dimethylamino)ethyl)acetamidyl calix4arene.
MDL No. :MFCD28396412
InChI Key :CQVAQQNDZCZBSU-UHFFFAOYSA-N
Pubchem ID :11953346

Safety of OTX008

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

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
CAL-62 30 µM 72 hours Evaluate the effect of OTX008 on cell proliferation, IC50 was 30 µM Cells. 2021 May 5;10(5):1112.
TT2609C02 1.1 µM 72 hours Evaluate the effect of OTX008 on cell proliferation, IC50 was 1.1 µM Cells. 2021 May 5;10(5):1112.
FTC133 0.3 µM 72 hours Evaluate the effect of OTX008 on cell proliferation, IC50 was 0.3 µM Cells. 2021 May 5;10(5):1112.
BCPAP 0.5 µM 72 hours Evaluate the effect of OTX008 on cell proliferation, IC50 was 0.5 µM Cells. 2021 May 5;10(5):1112.
TPC-1 0.2 µM 72 hours Evaluate the effect of OTX008 on cell proliferation, IC50 was 0.2 µM Cells. 2021 May 5;10(5):1112.
8505c 0.3 µM 72 hours Evaluate the effect of OTX008 on cell proliferation, IC50 was 0.3 µM Cells. 2021 May 5;10(5):1112.
SNU449 20 µM 48 hours To evaluate the effect of OTX008 on the viability of SNU449 cells. Results showed that OTX008 significantly inhibited cell viability at 20 µM concentration. Mol Oncol. 2022 Mar;16(5):1091-1118.
SNU387 20 µM 48 hours To evaluate the effect of OTX008 on the viability of SNU387 cells. Results showed that OTX008 significantly inhibited cell viability at 20 µM concentration. Mol Oncol. 2022 Mar;16(5):1091-1118.
HLE 20 µM 72 hours To evaluate the effect of OTX008 on the viability of HLE cells. Results showed that OTX008 significantly inhibited cell viability at 20 µM concentration. Mol Oncol. 2022 Mar;16(5):1091-1118.
PLC/PRF/5 20 µM 72 hours To evaluate the effect of OTX008 on the viability of PLC/PRF/5 cells. Results showed that OTX008 significantly inhibited cell viability at 20 µM concentration. Mol Oncol. 2022 Mar;16(5):1091-1118.
MHCC97L 50 μM OTX008 significantly inhibited the proliferation, migration and invasion of MHCC97L cells J Exp Clin Cancer Res. 2019 Oct 22;38(1):423.
HL7702 liver cells 10 μmol/L 3 hours Pretreatment with OTX008 for 3 hours could partially reverse and abolish the DBDCT-associated cytotoxicity, indicating that Gal-1 might be identified as a possible potential target for toxicity and bioactivity. Bioinorg Chem Appl. 2022 Feb 1;2022:5176300.
H9c2 cells 2.5–1.25–0.75 µM 6 days Evaluated the effect of OTX008 alone or combined with SBECD on H9c2 cell viability under hyperglycemic conditions, showing no toxicity and significantly improved cell survival. Pharmaceuticals (Basel). 2024 Jan 12;17(1):107.
ARPE-19 cells 2.5 μM, 5 μM, 10 μM 6 days OTX008 5 μM and 10 μM improved cell viability and markedly reduced galectin-1 protein expression in cells exposed to high glucose. Molecules. 2022 Jul 26;27(15):4785.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice 8505c xenograft model Intraperitoneal injection 5 mg/kg/day 5 days/week for 3 weeks Evaluate the effect of OTX008 on tumor growth and lung metastasis, results showed significant reduction in tumor volume Cells. 2021 May 5;10(5):1112.
BALB/c nude mice Subcutaneous injection and orthotopic implantation model Intraperitoneal injection 5 mg/3 days Every 3 days until the end of the experiment OTX008 alone or in combination with sorafenib significantly inhibited tumor growth and metastasis J Exp Clin Cancer Res. 2019 Oct 22;38(1):423.
Nude mice SQ20B and HEp-2 tumor models Intraperitoneal injection 10 mg/kg Once daily for 21 days OTX008 reduced tumor growth by an average of 25% in the SQ20B model, up to 35% on certain days. The effect was less pronounced in the HEp-2 model, whereas Avastin caused tumor growth stabilization. Int J Mol Sci. 2017 Dec 9;18(12):2671

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01724320 Solid Tumors PHASE1 UNKNOWN 2025-05-13 Institut Jules Bordet, Brussel... More >>s, 1000, Belgium|Hopital Beaujon - AP-HP, Clichy, 92110, France|Institut Claudius Regaud, Toulouse, 31052, France Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.07mL

0.21mL

0.11mL

5.34mL

1.07mL

0.53mL

10.67mL

2.13mL

1.07mL

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