ARQ 621
- Product Name
- ARQ 621
- CAS No.
- 1095253-39-6
- Chemical Name
- ARQ 621
- Synonyms
- ARQ 621;ARQ-621;ARQ621;ARQ 621 USP/EP/BP;motor,inhibit,cell,ARQ 621,division,protein,Inhibitor,microtubule,ARQ621,Kinesin,Anti-tumor,Eg5,ARQ-621;(R)-N-(3-Aminopropyl)-3-chloro-N-(1-(7-chloro-4-oxo-3-(phenylamino)-3,4-dihydroquinazolin-2-yl)but-3-yn-1-yl)-2-fluorobenzamide;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-
- CBNumber
- CB72627336
- Molecular Formula
- C28H24Cl2FN5O2
- Formula Weight
- 552.43
- MOL File
- 1095253-39-6.mol
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..…
N-Bromosuccinimide Price
- Product number
- B6039
- Product name
- ARQ621
- Packaging
- 5mg
- Price
- $296
- Updated
- 2021/12/16
- Product number
- B6039
- Product name
- ARQ621
- Packaging
- 25mg
- Price
- $747
- Updated
- 2021/12/16
- Product number
- DC7820
- Product name
- ARQ621
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1450
- Updated
- 2021/12/16
- Product number
- DC7820
- Product name
- ARQ621
- Purity
- >98%
- Packaging
- 1g
- Price
- $2900
- Updated
- 2021/12/16
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.
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