OTX008
Based on 18 publication(s) in Google Scholar
OTX008 is a selective inhibitor of galectin-1.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 286936-40-1
- Formula: C52H72N8O8
- Molecular Weight:937.18
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) OTX008
More- Adv Sci (Weinh). 2025 Jan 24:e2408788. [Abstract]
- Theranostics. 2024 Jan 1;14(2):843-860. [Abstract]
- Biomark Res. 2026 Jan 15;14(1):11. [Abstract]
- J Immunother Cancer. 2023 Aug;11(8):e007286. [Abstract]
- Cancer Lett. 2020 Jan 28;469:287-300. [Abstract]
- Cell Rep. 2021 Aug 31;36(9):109647. [Abstract]
- J Med Chem. 2023 Dec 28;66(24):16980-16990. [Abstract]
- Mol Ther Nucleic Acids. 2023 Jul 19:33:430-443. [Abstract]
- Cells. 2021 May 5;10(5):1112. [Abstract]
- Int J Mol Sci. 2024 Jun 19;25(12):6756. [Abstract]
- Int Immunopharmacol. 2025 May 15:158:114835. [Abstract]
- FEBS J. 2025 Dec;292(23):6211-6232. [Abstract]
- iScience. 2023 Mar 11;26(4):106385. [Abstract]
- bioRxiv. 2026 Jun 7:2026.06.03.729765. [Abstract]
- bioRxiv. 2026 Jun 19.
- University of California, Los Angeles. 2026.
- bioRxiv. 2026 Feb 23.
- Patent. US20250228801A1.
Customer Validation & Images
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In Vivo Efficacy Study
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Flow Cytometry
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IHC
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Flow Cytometry
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Bio/Physico-chemical Assay
All Galectin Isoforms
More
Biological Activity
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Galectin-1 |
Growth inhibitory concentrations (GI50) of OTX008 in a large panel of human solid tumour cell lines ranges from 3 to 500 μM. A significant correlation between OTX008 GI50 values and Gal1 mRNA (LGALS1) and protein expression levels in the panel of cancer cells is observed. In SQ20B and A2780-1A9 cells, OTX008 inhibits Gal1 expression and ERK1/2 and AKT-dependent survival pathways, and induces G2/M cell cycle arrest through CDK1. OTX008 enhances the anti-proliferative effects of Semaphorin-3A (Sema3A) in SQ20B cells and reverses invasion induced by exogenous Gal1[1]. OTX008 affects endothelial cell proliferation, motility, invasiveness, and cord formation. Tumor cell proliferation is also inhibited, with differences in sensitivity among cell lines (IC50 from 1 to 190 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 286936-40-1
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Appearance Solid
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Molecular Weight 937.18
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Formula C52H72N8O8
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Color White to off-white
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SMILES
O=C(NCCN(C)C)COC1=C(C2)C=CC=C1CC3=C(OCC(NCCN(C)C)=O)C(CC4=CC=CC(CC5=CC=CC2=C5OCC(NCCN(C)C)=O)=C4OCC(NCCN(C)C)=O)=CC=C3
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Synonyms
Calixarene 0118; PTX008
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (18)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Galectin-1-Induced Tumor Associated Macrophages Repress Antitumor Immunity in Hepatocellular Carcinoma Through Recruitment of Tregs. [Abstract]2025 Jan 24:e2408788. PMID: 39853961
OTX008 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jan 24:e2408788. [Abstract]
Gal1 inhibitor OTX008（5 mg/kg; i.p.; every 3 days) exhibited a pronounced inhibition of tumor growth and a notable enhancement in survival of orthotopic mouse models of HCC (hepatocellular carcinoma).
OTX008 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jan 24:e2408788. [Abstract]
OTX008（5 mg/kg; i.p.; every 3 days) effectively suppressed the secretion of CCL20 by TAMs, which subsequently decreased the recruitment of CCR6+ Tregs and the proportion of Tregs in the TME of orthotopic mouse models of HCC (hepatocellular carcinoma).
OTX008 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jan 24:e2408788. [Abstract]
Representative IHC staining images (upper) and quantification (lower) of Foxp3+ and CD8+ cells in the orthotopic mouse models of HCC (hepatocellular carcinoma) treated with OTX008（5 mg/kg; i.p.; every 3 days).
OTX008 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jan 24:e2408788. [Abstract]
Intracellular staining of granzyme B, perforin, IFN‐γ and TNF‐α in CD8+ T cells in the orthotopic mouse models of HCC (hepatocellular carcinoma) treated with OTX008（5 mg/kg; i.p.; every 3 days).
OTX008 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jan 24:e2408788. [Abstract]
OTX008 (50 μg/mL; 48 h; 37 ℃) decreased the expression and secretion of CCL20 in BMDMs incubated with shNC hepa1-6 cells.
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Theranostics
Comprehensive characterization of early-programmed tumor microenvironment by tumor-associated macrophages reveals galectin-1 as an immune modulatory target in breast cancer. [Abstract]2024 Jan 1;14(2):843-860. PMID: 38169569 -
Biomark Res
miR-22-Galectin-1 as an integral signaling axis in regulating metabolism and immunity in HCC. [Abstract]2026 Jan 15;14(1):11. PMID: 41540504 -
J Immunother Cancer
2023 Aug;11(8):e007286. PMID: 37586772 -
Cancer Lett
RACK1 promotes the invasive activities and lymph node metastasis of cervical cancer via galectin-1. [Abstract]2020 Jan 28;469:287-300. PMID: 31705928 -
Cell Rep
2021 Aug 31;36(9):109647. PMID: 34469737 -
J Med Chem
2023 Dec 28;66(24):16980-16990. PMID: 38059452 -
Mol Ther Nucleic Acids
Chloroquine and cytosolic galectins affect endosomal escape of antisense oligonucleotides after Stabilin-mediated endocytosis. [Abstract]2023 Jul 19:33:430-443. PMID: 37575283 -
Cells
2021 May 5;10(5):1112. PMID: 34063063 -
Int J Mol Sci
A Quantitative Human Red Blood Cell Agglutination Assay for Characterisation of Galectin Inhibitors. [Abstract]2024 Jun 19;25(12):6756. PMID: 38928462 -
Int Immunopharmacol
Galectin-1: An important regulator in myeloid differentiation and acute myeloid leukemia as well as a promising prognostic indicator and therapeutic target. [Abstract]2025 May 15:158:114835. PMID: 40378432 -
FEBS J
Gal-1 promotes lung cancer cell survival by enhancing PARP1/H1.2 interaction to promote DNA repair upon DNA damage response. [Abstract]2025 Dec;292(23):6211-6232. PMID: 40365664 -
iScience
Niche-expressed Galectin-1 is involved in pre-B acute lymphoblastic leukemia relapse through pre-B cell receptor activation. [Abstract]2023 Mar 11;26(4):106385. PMID: 37009219 -
bioRxiv
2026 Jun 7:2026.06.03.729765. PMID: 42282633 -
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Solvent & Solubility
Ethanol : 33.33 mg/mL (35.56 mM; Need ultrasonic)
DMSO : 5 mg/mL (5.34 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% EtOH 90% Saline
Solubility: ≥ 1.25 mg/mL (1.33 mM); Clear solution
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (0.53 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (0.53 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 0.5 mg/mL (0.53 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Mice[1]
A total of 8×106 A2780-1A9 ovarian cells are injected subcutaneously into the right lateral flank of female nu/nu athymic mice. Once tumours are palpable (50 mm3), mice are randomised to receive treatment intraperitoneally with either PBS (3 times/week), 5 mg/kg OTX008 (3 times/week), 6 mg/kg cisplatin (days 1, 8 and 15) or 10 mg/kg docetaxel (days 1, 8 and 15). Tumour size was measured twice weekly with calipers and tumour volume is calculated as 3.14×(width2)/length[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Astorgues-Xerri L, et al. OTX008, a selective small-molecule inhibitor of galectin-1, downregulates cancer cell proliferation, invasion and tumour angiogenesis. Eur J Cancer. 2014 Sep;50(14):2463-77. [Content Brief]
[2]. Zucchetti M, et al. Pharmacokinetics and antineoplastic activity of galectin-1-targeting OTX008 in combination with sunitinib. Cancer Chemother Pharmacol. 2013 Oct;72(4):879-87. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Ethanol | 1 mM | 1.0670 mL | 5.3352 mL | 10.6703 mL | 26.6758 mL |
| 5 mM | 0.2134 mL | 1.0670 mL | 2.1341 mL | 5.3352 mL | |
| Ethanol | 10 mM | 0.1067 mL | 0.5335 mL | 1.0670 mL | 2.6676 mL |
| 15 mM | 0.0711 mL | 0.3557 mL | 0.7114 mL | 1.7784 mL | |
| 20 mM | 0.0534 mL | 0.2668 mL | 0.5335 mL | 1.3338 mL | |
| 25 mM | 0.0427 mL | 0.2134 mL | 0.4268 mL | 1.0670 mL | |
| 30 mM | 0.0356 mL | 0.1778 mL | 0.3557 mL | 0.8892 mL |
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