EC0489

Name: EC0489
Brand: TargetMol
SKU: T13672
Rating: 4.5 (1 reviews)

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Catalog No. T13672Cas No. 1096702-14-5

EC0489 is a small molecule-drug conjugate (SMDC) that combines folic acid and desacetyl vinblastine hydrazide, serving as a high-affinity ligand for the folate receptor (FR) in refractory or metastatic tumors.

EC0489

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Catalog No. T13672Cas No. 1096702-14-5

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
25 mg	Inquiry	Inquiry	Inquiry

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Product Introduction

Bioactivity

Description	EC0489 is a small molecule-drug conjugate (SMDC) that combines folic acid and desacetyl vinblastine hydrazide, serving as a high-affinity ligand for the folate receptor (FR) in refractory or metastatic tumors.
In vitro	FR-positive KB cells are highly sensitive to EC0489 with an IC50 of 5 nM.The affinity of EC0489 toward the folate receptor (FR) is approximately half of that of folic acid (relative affinity 0.50).
In vivo	EC0489, administered at doses of 2, 3, and 4 μmol/kg, exhibits dose-dependent antitumor activity in mouse KB tumor models. Furthermore, EC0489 demonstrates a favorable toxicology profile in rats.

Chemical Properties

Molecular Weight	2550.7
Formula	C₁₁₁H₁₅₆N₂₂O₄₃S₂
Cas No.	1096702-14-5
Smiles	[H][C@@]12N3CC[C@@]11c4cc(c(OC)cc4N(C)[C@@]1([H])[C@](O)([C@H](O)[C@]2(CC)C=CC3)C(=O)NNC(=O)OCCSSC[C@H](NC(=O)[C@H](CCC(=O)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(=O)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(=O)NC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO)NC(=O)CC[C@H](NC(=O)c1ccc(NCc2c[nH]c3nc(N)nc(=O)c3n2)cc1)C(O)=O)C(O)=O)[C@]1(C[C@@]2([H])C[N@](C[C@](O)(CC)C2)CCc2c1[nH]c1ccccc21)C(=O)OC \|c:29\|
Relative Density.	1.66 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc