Endostatin Human

Endostatin Human Recombinant
Cat. No.
BT6509
Source
E.coli.
Synonyms
Appearance
Sterile filtered liquid formulation.
Purity
Greater than 95.0% as determined by SDS-PAGE.
Usage
Prospec's products are furnished for LABORATORY RESEARCH USE ONLY. The product may not be used as drugs, agricultural or pesticidal products, food additives or household chemicals.
Shipped with Ice Packs
In Stock

Description

Endostatin Human Recombinant produced in E.Coli is a single, non-glycosylated, polypeptide having a predicted molecular mass of 20kDa.
C-terminal fragment of collagen XVIII that has been shown to act as a potent inhibitor of angiogenesis and tumor growth in vitro and in vivo. Induces tyrosine phosphorylation of Shc (SH2 domain adapter protein) leading to specific inhibition in endothelial cell proliferation.
The Endostatin is purified by proprietary chromatographic techniques.

Product Specs

Introduction
Cancer cell clusters require a dedicated blood supply to grow beyond 1-2 mm in diameter. This is because diffusion alone becomes insufficient to provide adequate oxygen and nutrients or remove waste products. To overcome this limitation, cancer cells release substances that promote the formation of new blood vessels, a process called angiogenesis. Angiogenesis is essential for the growth and survival of solid tumors and their metastases. Tumors upregulate the production of various angiogenic factors, such as FGF-a, FGF-b, VEGF, and VPF, to stimulate angiogenesis. However, many malignant tumors also produce angiogenesis inhibitors, including angiostatin and thrombospondin. The angiogenic phenotype results from the balance between these positive and negative regulators of neovascularization. Endostatin acts as an effective angiogenesis inhibitor by preventing the proliferation of endothelial cells.
Description
Recombinant Human Endostatin, produced in E. coli, is a single, non-glycosylated polypeptide with an expected molecular weight of 20 kDa. This C-terminal fragment of collagen XVIII exhibits potent angiogenesis and tumor growth inhibition both in vitro and in vivo. It functions by inducing tyrosine phosphorylation of Shc, an SH2 domain adapter protein, leading to the specific inhibition of endothelial cell proliferation. Purification of Endostatin is achieved through proprietary chromatographic techniques.
Physical Appearance
Sterile, filtered liquid solution.
Formulation
Recombinant Human Endostatin is supplied in a 30mM Sodium acetate buffer with Mannitol, adjusted to pH 5.5.
Stability
Endostatin should be stored at a temperature range of 2-8°C. It is crucial to avoid freezing.
Purity
SDS-PAGE analysis indicates a purity exceeding 95.0%.
Biological Activity
The measured biological activity is 16,000 IU/mg.
Source
E.coli.

Product Science Overview

Discovery and Mechanism of Action

Endostatin was initially isolated in Dr. Judah Folkman’s lab, a pioneer in the field of angiogenesis research . The protein is produced by the proteolytic cleavage of collagen XVIII by enzymes such as cathepsins . Its anti-angiogenic activity is attributed to its ability to inhibit endothelial cell proliferation, migration, and tube formation, which are essential steps in the angiogenesis process .

Clinical Development and Applications

The recombinant form of endostatin (rh-endostatin) has been developed to enhance its stability and solubility for clinical use . Early studies demonstrated that continuous low-dose administration of rh-endostatin was more effective than intermittent dosing in preclinical models . This led to the development of various administration protocols, including continuous intravenous infusion followed by subcutaneous injections .

Clinical Trials and Effectiveness

Several clinical trials have been conducted to evaluate the safety and efficacy of rh-endostatin in cancer treatment. A phase I study demonstrated that rh-endostatin could be safely administered both by continuous infusion and by twice-daily subcutaneous injections up to 120 mg/m²/day . The pharmacokinetic profile showed predictable serum concentrations, and the target endostatin levels were achieved at doses of 60 mg/m²/day and above .

In a more recent study, rh-endostatin combined with PD-1 inhibitors and chemotherapy showed promising results as a first-line treatment for advanced or metastatic non-small cell lung cancer (NSCLC) . The combination therapy yielded favorable effectiveness with a manageable safety profile, representing a promising treatment modality for patients with advanced cancer .

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