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EMD534085

Name: EMD534085
Brand: TargetMol
SKU: TQ0314
Rating: 4.5 (1 reviews)

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Catalog No. TQ0314Cas No. 858668-07-2

EMD534085 is an effective and selective mitotic kinesin-5 inhibitor (IC50: 8 nM).

EMD534085

😃Good

Catalog No. TQ0314Cas No. 858668-07-2

EMD534085 is an effective and selective mitotic kinesin-5 inhibitor (IC50: 8 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
500 μg	$142	35 days	35 days
1 mg	$258	35 days	35 days
5 mg	$1,130	35 days	35 days
10 mg	$1,980	35 days	35 days

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

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	EMD534085 is an effective and selective mitotic kinesin-5 inhibitor (IC50: 8 nM).
Targets&IC50	Kinesin-5:8 nM
In vitro	EMD 534085 does not inhibit other tested kinesins at 1 μM or 10 μM concentrations, showing selectivity for kinesin-5. EMD 534085 binds to the allosteric pocket of kinesin-5 [1]. It induces rapid cell death in HL60 cells during mitotic arrest, activating caspase-8, -9, -3, -7; cleaving Parp1; and degrading Mcl1 and XIAP. Additionally, EMD 534085-treated HL60 cells exhibit a significantly increased phospho-histone H3 level starting 6 hours post thymidine release [2].
In vivo	In a pharmacokinetic study of EMD 534085 conducted at a low dose in mice, average clearance was observed at 1.8 L/h/kg, with a volume of distribution of 7.4 L/kg and a half-life approximately 2.5 hours. High dose experiments (>10 mg/kg) consistently demonstrated a bioavailability exceeding 50% in mice. Intraperitoneal administration of EMD 534085 resulted in significant systemic exposure, contributing to a notable reduction in tumor growth without inducing toxic side effects [1].
Cell Research	Epithelial cell lines HeLa and MCF7 are synchronized in G2-phase using RO-3306. Cells are treated with 10 μM RO-3306 for 16 hrs, and then are ished and released to either warm growth medium or medium supplemented with 500 nM EMD534085 [2].

Chemical Properties

Molecular Weight	476.53
Formula	C₂₅H₃₁F₃N₄O₂
Cas No.	858668-07-2
Smiles	[H][C@@]12CC[C@H](CNC(=O)NCCN(C)C)O[C@]1([H])c1cc(ccc1N[C@H]2c1ccccc1)C(F)(F)F
Relative Density.	1.195 g/cm3

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.

Solubility Information

DMSO: 25 mg/mL (52.46 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0985 mL	10.4925 mL	20.9850 mL	104.9252 mL
5 mM	0.4197 mL	2.0985 mL	4.1970 mL	20.9850 mL
10 mM	0.2099 mL	1.0493 mL	2.0985 mL	10.4925 mL
20 mM	0.1049 mL	0.5246 mL	1.0493 mL	5.2463 mL
50 mM	0.0420 mL	0.2099 mL	0.4197 mL	2.0985 mL

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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