[CAS NO. 286936-40-1] OTX008
PRODUCTS SPECIFICATIONS [286936-40-1]
DESCRIPTION [286936-40-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 937.18 |
| Molecular Formula | C52H72N8O8 |
| 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 |
3 Publications Citing Use of MCE
Summary
OTX008 is a selective inhibitor of galectin-1 .
IC50 & Target
Galectin-1 [1] .
In Vitro
Growth inhibitory concentrations (GI 50 ) of OTX008 in a large panel of human solid tumour cell lines ranges from 3 to 500 μM. A significant correlation between OTX008 GI 50 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 (IC 50 from 1 to 190 μM) [2] .
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01724320 | Oncoethix GmbH |
Solid Tumors
|
February 2012 | Phase 1 |
Appearance
Solid
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
Ethanol : 12.5 mg/mL ( 13.34 mM ; Need ultrasonic)
DMSO : 6.25 mg/mL ( 6.67 mM ; ultrasonic and warming and heat to 60°C)
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 |
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1.
Add each solvent one by one: 10% EtOH >> 90% Saline
Solubility: ≥ 1.25 mg/mL (1.33 mM); Clear solution
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2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1 mg/mL (1.07 mM); Clear solution
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4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1 mg/mL (1.07 mM); Clear solution
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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
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.
- [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.
