product name ARQ 621
Description: ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Eg5 is essential for the dynamic organization of the mitotic spindle. Over-expression of Eg5 leads to genomic instability and tumor formation. Over-expression of Eg5 causes genomic instability and tumor formation in mice; therefore, Eg5 is a potential anti-cancer target. Preclinical data shows anti-tumor activity of ARQ 621 across a wide range of cell lines from human solid and hematological malignancies.
References: Rosen L, et al. Annual Meeting of ASCO: abstract 3076
552.43
Formula
C28H24Cl2FN5O2
CAS No.
1095253-39-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (181.0 mM)
Water: <1 mg/mL
Ethanol: 100 mg/mL (181.0 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
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| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Rosen L, et al. Annual Meeting of ASCO: abstract 3076. |
