ARQ 621

Catalog No.S7355

For research use only.

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

ARQ 621 Chemical Structure

CAS No. 1095253-39-6

Selleck's ARQ 621 has been cited by 3 Publications

Purity & Quality Control

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Biological Activity

Description ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1.
Targets
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 ARQ 621, there is no envidence of bone marrow toxicity in pre-clinical mouse efficacy models or safety studies in rats and dogs. [1]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(181.01 mM)
Ethanol 100 mg/mL
(181.01 mM)
Water Insoluble

Chemical Information

Molecular Weight 552.43
Formula

C28H24Cl2FN5O2

CAS No. 1095253-39-6
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00825487 Completed Drug: ARQ 621 Metastatic Solid Tumors Refractory/Relapsed Hematologic Malignancies ArQule Inc. (a wholly owned subsidiary of Merck Sharp and Dohme a subsidiary of Merck & Co. Inc.) August 2009 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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