For research use only. Not for therapeutic Use.
ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity[1]. ARQ 621 is a kinesin inhibitor[2]. ARQ 621 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Over-expression of Eg5 causes genomic instability and tumor formation in mice; therefore, Eg5 is a potential anti-cancer target[1].
| Catalog Number | I002796 |
| CAS Number | 1095253-39-6 |
| Synonyms | N-(3-aminopropyl)-N-[(1R)-1-(3-anilino-7-chloro-4-oxoquinazolin-2-yl)but-3-ynyl]-3-chloro-2-fluorobenzamide |
| Molecular Formula | C28H24Cl2FN5O2 |
| Purity | ≥95% |
| InChI | 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 |
| InChIKey | UPJSUQWHUVLLNW-XMMPIXPASA-N |
| 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 |
| Reference | [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. |
