ARQ 621 Property

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)

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

H400Very toxic to aquatic life

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P273Avoid release to the environment.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P391Collect spillage. Hazardous to the aquatic environment

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

ARQ 621 Chemical Properties,Usage,Production

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.