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| ARQ 621 Basic information |
| Product Name: | ARQ 621 | | Synonyms: | ARQ 621;N-(3-aminopropyl)-3-chloro-N-[(1R)-1-[7-chloro-3,4-dihydro-4-oxo-3-(phenylamino)-2-quinazolinyl]-3-butyn-1-yl]-2-fluoro-benzamide;ARQ-621;ARQ621;Benzamide, N-(3-aminopropyl)-3-chloro-N-[(1R)-1-[7-chloro-3,4-dihydro-4-oxo-3-(phenylamino)-2-quinazolinyl]-3-butyn-1-yl]-2-fluoro-;ARQ 621 USP/EP/BP | | CAS: | 1095253-39-6 | | MF: | C28H24Cl2FN5O2 | | MW: | 552.43 | | EINECS: | | Product Categories: | Inhibitors | | Mol File: | 1095253-39-6.mol |
| ARQ 621 Chemical Properties |
| Boiling point | 730.6±70.0 °C(Predicted) | | density | 1.34±0.1 g/cm3(Predicted) | | solubility | Soluble in DMSO | | pka | 9.40±0.10(Predicted) |
| ARQ 621 Usage And Synthesis |
| Biological Activity | arq 621 is a novel, allosteric,potent and selective inhibitor of eg5. eg5 is a member of the mitotickinesin superfamily which plays a key role in mitosis. eg5 is essential for the dynamic organization of the mitotic spindle. over-expression of eg5 leads to genomic instability and tumor formation [1]. | | in vitro | in human liver microsomes, t1/2 of arq 621 was 53 min. the t1/2value of arq 621 in male and female mouse, rat, dog and monkey liver microsomes was 43, 53, 56, 53, 47, 44, 36, and 32 minutes, respectively [1]. ic50value of arq 621 for cyp 1a2, 2c9, 2d6, 3a4, 2c19, and 2c8 was>20, >20, >20, 4.1, 4.0, and 15 μm, respectively. arq 621 showed anti-tumor activity with potencies in the low nanomolar range across a range of human solid and hematological malignanciescancer cell types such as colon, nsclc, gastric, and hematologic cancer cell lines [1]. | | in vivo | oral administration of arq 621 showed that the bioavailability of arq 621 was approximately 9% [1]. | | references | savage r e, zhong c, hall t, et al. in vitro adme properties of arq 621: a specific eg5 inhibitor[j]. cancer research, 2010, 70(8 supplement): 5783-5783.rosen l, chen l c, iyengar t, et al. arq 621, a novel potent and selective inhibitor of eg5: preclinical data and early results from a clinical phase 1 study[j]. cancer research, 2010, 70(8 supplement): 2750-2750.chen l c, rosen l s, iyengar t, et al. first-in-human study with arq 621, a novel inhibitor of eg5: final results from the solid tumors cohort[c]//asco annual meeting proceedings. 2011, 29(15_suppl): 3076. |
| ARQ 621 Preparation Products And Raw materials |
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