ARQ 621

Alias: ARQ621; ARQ 621; ARQ-621
Cat No.:V1631 Purity: ≥98%
ARQ 621 (ARQ-621; ARQ621) is an allosteric Eg5 mitotic motor protein inhibitor with potential anticancer activity.
ARQ 621 Chemical Structure CAS No.: 1095253-39-6
Product category: Kinesin
This product is for research use only, not for human use. We do not sell to patients.
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5mg
10mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

ARQ 621 (ARQ-621; ARQ621) is an allosteric Eg5 mitotic motor protein inhibitor with potential anticancer activity. Eg5 is overexpressed in many cancer tumors and is important for the dynamic organization of the mitotic spindle, thus has become an excellent target of anticancer therapeutics.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Eg5 is a putative anti-cancer target since over-expression of the protein results in genomic instability and tumor development in mice[1].
ln 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.
Animal Protocol


References
[1]. L. C. Chen, et al. First-in-human study with ARQ 621, a novel inhibitor of Eg5: Final results from the solid tumors cohort.J Clin Oncol. 2011, May (20): 3076-3076.
[2]. Lindsay S Roberts, et al. Mapping Novel Metabolic Nodes Targeted by Anti-Cancer Drugs that Impair Triple-Negative Breast Cancer Pathogenicity. ACS Chem Biol. 2017 Apr 21;12(4):1133-1140.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C28H24CL2FN5O2
Molecular Weight
552.43
CAS #
1095253-39-6
SMILES
C#CC[C@H](C1=NC2=C(C=CC(=C2)Cl)C(=O)N1NC3=CC=CC=C3)N(CCCN)C(=O)C4=C(C(=CC=C4)Cl)F
InChi Key
UPJSUQWHUVLLNW-XMMPIXPASA-N
InChi Code
InChI=1S/C28H24Cl2FN5O2/c1-2-8-24(35(16-7-15-32)27(37)21-11-6-12-22(30)25(21)31)26-33-23-17-18(29)13-14-20(23)28(38)36(26)34-19-9-4-3-5-10-19/h1,3-6,9-14,17,24,34H,7-8,15-16,32H2/t24-/m1/s1
Chemical Name
(R)-N-(3-aminopropyl)-3-chloro-N-(1-(7-chloro-4-oxo-3-(phenylamino)-3,4-dihydroquinazolin-2-yl)but-3-yn-1-yl)-2-fluorobenzamide
Synonyms
ARQ621; ARQ 621; ARQ-621
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 100 mg/mL (181.0 mM)
Water:<1 mg/mL
Ethanol:100 mg/mL (181.0 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.8102 mL 9.0509 mL 18.1018 mL
5 mM 0.3620 mL 1.8102 mL 3.6204 mL
10 mM 0.1810 mL 0.9051 mL 1.8102 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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