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CW069

Cat. No. M10666
CW069 Structure
Synonym:

CW-069

Size Price Availability Quantity
5mg USD 134  USD134 In stock
10mg USD 222  USD222 In stock
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Quality Control & Documentation
Biological Activity

CW069 is an allosteric inhibitor of HSET with IC50 of 75 μM, it showed marked activity against HSET in vitro. CW069 therefore constitutes a valuable tool for probing HSET function and, by reducing the growth of cells containing supernumerary centrosomes, paves the way for new cancer therapeutics. CW-069 potently suppresses N1E-115 cells, and less potently inhibits the NHDF cells, with IC50 of 86 ± 10 μM and 181 ± 7 μM, respectively. CW-069 (100 or 200 μM) causes increased multipolar spindles in N1E-115 cells with supernumerary centrosomes and shows no effect on altering bipolar spindle morphology in normal human dermal fibroblast cells. CW-069 (200 μM) cacuses multipolar anaphase and cell death induced in N1E-115 cells via transfection with HSET siRNA, and antagonizes inhibition of KSP by monastrol, but does not exert mitotic arrest in HeLa cells.

Chemical Information
Molecular Weight 500.33
Formula C23H21IN2O3
CAS Number 1594094-64-0
Solubility (25°C) DMSO ≥ 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] D Bhakta-Guha, et al. Curr Med Chem . Dis-organizing centrosomal clusters: specific cancer therapy for a generic spread?

[2] Ciorsdaidh A Watts, et al. Chem Biol . Design, synthesis, and biological evaluation of an allosteric inhibitor of HSET that targets cancer cells with supernumerary centrosomes

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Keywords: CW069, CW-069 supplier, Kinesin, inhibitors, activators

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