1. Immunology/Inflammation
  2. Galectin
  3. OTX008

OTX008  (Synonyms: Calixarene 0118; PTX008)

Cat. No.: HY-19756 Purity: 99.09%
COA Handling Instructions

OTX008 is a selective inhibitor of galectin-1.

For research use only. We do not sell to patients.

OTX008 Chemical Structure

OTX008 Chemical Structure

CAS No. : 286936-40-1

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Customer Review

Based on 8 publication(s) in Google Scholar

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Description

OTX008 is a selective inhibitor of galectin-1.

IC50 & Target

Galectin-1

 

In Vitro

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.

In Vivo

OTX008 inhibits growth of A2780-1A9 xenografts. OTX008 treatment is associated with down-regulation of Gal1 and Ki67 in treated tumours, as well as decreased microvessel density and VEGFR2 expression. Finally, combination studies show OTX008 synergy with several cytotoxic and targeted therapies, principally when OTX008 is administered first[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

937.18

Formula

C52H72N8O8

CAS No.
Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0670 mL 5.3352 mL 10.6703 mL
5 mM 0.2134 mL 1.0670 mL 2.1341 mL
10 mM 0.1067 mL 0.5335 mL 1.0670 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% EtOH    90% Saline

    Solubility: ≥ 1.25 mg/mL (1.33 mM); Clear solution

  • 2.

    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

  • 3.

    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

  • 4.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 0.5 mg/mL (0.53 mM); Clear solution

  • 5.

    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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.09%

References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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OTX008 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
OTX008
Cat. No.:
HY-19756
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