| Identification | Back Directory | [Name]
ARQ 621 | [CAS]
1095253-39-6 | [Synonyms]
ARQ 621
ARQ-621;ARQ621
ARQ 621 USP/EP/BP
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
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- | [Molecular Formula]
C28H24Cl2FN5O2 | [MDL Number]
MFCD25976786 | [MOL File]
1095253-39-6.mol | [Molecular Weight]
552.43 |
| Chemical Properties | Back Directory | [Boiling point ]
730.6±70.0 °C(Predicted) | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Powder | [pka]
9.40±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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. | [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]. | [IC 50]
Eg5 | [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. |
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BOC Sciences
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NCE Biomedical Co.,Ltd.
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