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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
FTC133 0.3 µM 72 hours Evaluate the effect of OTX008 on cell proliferation, IC50 was 0.3 µM PMC8147933
CAL-62 30 µM 72 hours Evaluate the effect of OTX008 on cell proliferation, IC50 was 30 µM PMC8147933
BCPAP 0.5 µM 72 hours Evaluate the effect of OTX008 on cell proliferation, IC50 was 0.5 µM PMC8147933
TPC-1 0.2 µM 72 hours Evaluate the effect of OTX008 on cell proliferation, IC50 was 0.2 µM PMC8147933
8505c 0.3 µM 72 hours Evaluate the effect of OTX008 on cell proliferation, IC50 was 0.3 µM PMC8147933
TT2609C02 1.1 µM 72 hours Evaluate the effect of OTX008 on cell proliferation, IC50 was 1.1 µM PMC8147933
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. PMC8895452
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. PMC8895452
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. PMC8895452
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. PMC8895452
MHCC97L 50 μM OTX008 significantly inhibited the proliferation, migration and invasion of MHCC97L cells PMC6805403
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. PMC8824758
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. PMC10819853
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. PMC9332238

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 PMC8147933
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 PMC6805403
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. PMC5751273

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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