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OTX008 (Synonyms: Calixarene 0118; PTX008)

Cat. No.: HY-19756
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

Size Price Stock
5 mg USD 190 Get quote
10 mg USD 290 Get quote
25 mg USD 590 Get quote
50 mg USD 990 Get quote
100 mg USD 1650 Get quote

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

OTX008 is a selective inhibitor of galectin-1.

IC50 & Target

Galectin-1[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].

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

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.
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
Molecular Weight

937.18

Formula

C₅₂H₇₂N₈O₈

CAS No.

286936-40-1

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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

Cat. No.: HY-19756