An inhibitor of Gal-1; decreases lactose binding to Gal-1 (Kds = 290 and 100 μM in the presence and absence of compound

OTX008 – 10 mg

Brand:
Cayman
CAS:
286936-40-1
Storage:
-20
UN-No:
Non-Hazardous - /

OTX008 is a small molecule topomimetic of the antiangiogenic peptide anginex and an inhibitor of galectin-1 (Gal-1).{41594} It decreases lactose binding to Gal-1 with Kd values of 290 and 100 μM in the presence and absence of OTX008, respectively, and is cytotoxic against a cancer cell panel with IC50 values that directly correlate to Gal-1 mRNA expression. OTX008 inhibits proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = 2 μM) and reduces HUVEC migration in a wound healing assay.{41595} OTX008 is angiostatic in a chorioallantoic membrane (CAM) assay, inducing formation of shorter, finer, and less defined vessels than vehicle control in fertilized chicken eggs. In vivo, OTX008 (2.4 and 10 mg/kg) reduces tumor growth in the MA148 ovarian mouse xenograft model and the B16 murine melanoma syngeneic model via decreases in tumor microvessel density and induction of apoptosis.  

 

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SKU: 23130 - 10 mg Category:

Description

An inhibitor of Gal-1; decreases lactose binding to Gal-1 (Kds = 290 and 100 μM in the presence and absence of compound, respectively); cytotoxic against a cancer cell panel with IC50 values that directly correlate to Gal-1 mRNA expression; inhibits proliferation of HUVECs (IC50 = 2 μM) and reduces HUVEC migration in a wound healing assay; reduces tumor growth in the MA148 ovarian mouse xenograft model and the B16 murine melanoma syngeneic model via decreases in tumor microvessel density and induction of apoptosis (2.4 and 10 mg/kg)

Formal name: 2,2′,2”,2”’-[pentacyclo[19.3.1.13,7.19,13.115,19]octacosa-1(25),3,5,7(28),9,11,13(27),15,17,19(26),21,23-dodecaene-25,26,27,28-tetrayltetrakis(oxy)]tetrakis[N-[2-(dimethylamino)ethyl]-acetamide

Synonyms:  Calixarene 0118|PTX008

Molecular weight: 937.2

CAS: 286936-40-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Death

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