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ARQ 621 Kinesin inhibitor

Name: ARQ 621
Brand: Selleck Chemicals
SKU: S7355
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S7355

ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1.

Chemical Structure

Molecular Weight: 552.43

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S735501 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 98.18%

98.18

Related Targets	Akt Microtubule Associated Wnt/beta-catenin HSP (HSP90) PKC Integrin Bcr-Abl Actin FAK ROCK PAK Dynamin MLCK MPS1 PORCN Gap-Junction Cardiac Myosin TACC3 Myosin
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Chemical Information, Storage & Stability

Molecular Weight	552.43	Formula	C₂₈H₂₄Cl₂FN₅O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1095253-39-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C#CCC(C1=NC2=C(C=CC(=C2)Cl)C(=O)N1NC3=CC=CC=C3)N(CCCN)C(=O)C4=C(C(=CC=C4)Cl)F

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (181.01 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (9.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.3mg/ml (0.54mM)	Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Eg5 mitotic motor protein ^[1]
In vitro	ARQ 621 demonstrates anti-tumor activity against a wide range of human cancer cell lines in vitro, including colon, lung, endometrial, bladder, and hematologic cancer cell lines, with significantly less cytotoxicity against hematopoietic cells. ^[1]
In vivo	ARQ 621, as a novel clinical stage drug candidate, inhibits a number of xenografts grown in athymic mice, such as pancreatic, breast, prostate, and ovarian carcinomas with no hematological changes. Furthermore, for this compound, there is no evidence of bone marrow toxicity in pre-clinical mouse efficacy models or safety studies in rats and dogs. ^[1]
References	http://meetinglibrary.asco.org/content/83067-102

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00825487	Completed	Metastatic Solid Tumors Refractory/Relapsed Hematologic Malignancies	ArQule Inc. a subsidiary of Merck Sharp & Dohme LLC a subsidiary of Merck & Co. Inc. (Rahway NJ USA)	August 2009	Phase 1

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