OTX008

OTX008 is a selective inhibitor of galectin-1.

Product information

CAS Number: 286936-40-1

Molecular Weight: 937.18

Formula: C52H72N8O8

Chemical Name: N-[2-(dimethylamino)ethyl]-2-{[26,27,28-tris({[2-(dimethylamino)ethyl]carbamoyl}methoxy)pentacyclo[19.3.1.1³,⁷.1⁹,¹³.1¹⁵,¹⁹]octacosa-1(25),3(28),4,6,9,11,13(27),15,17,19(26),21,23-dodecaen-25-yl]oxy}acetamide

Smiles: CN(C)CCNC(=O)COC1C2CC3C=CC=C(CC4C=CC=C(CC5=CC=CC(CC=1C=CC=2)=C5OCC(=O)NCCN(C)C)C=4OCC(=O)NCCN(C)C)C=3OCC(=O)NCCN(C)C

InChiKey: CQVAQQNDZCZBSU-UHFFFAOYSA-N

InChi: InChI=1S/C52H72N8O8/c1-57(2)25-21-53-45(61)33-65-49-37-13-9-14-38(49)30-40-16-11-18-42(51(40)67-35-47(63)55-23-27-59(5)6)32-44-20-12-19-43(52(44)68-36-48(64)56-24-28-60(7)8)31-41-17-10-15-39(29-37)50(41)66-34-46(62)54-22-26-58(3)4/h9-20H,21-36H2,1-8H3,(H,53,61)(H,54,62)(H,55,63)(H,56,64)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 10 mg/mL (10.67 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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).

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.

Products are for research use only. Not for human use.