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PHA-680632

Cat. No. M3552
PHA-680632 Structure
Size Price Availability Quantity
5mg USD 150  USD150 In stock
10mg USD 280  USD280 In stock
50mg USD 900  USD900 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

PHA-680632 is the first representative of a new class of Aurora inhibitors (Aurora A/B/C IC50 at 27, 135 and 120 nM, respectively). This agent has a high potential for further development as an anticancer therapeutic. PHA-680632 is active on a wide range of cancer cell lines and shows significant tumor growth inhibition in different animal tumor models at well-tolerated doses. The IC50 of PHA-680632 for cell anti-proliferation ranged from 0.11 uM to 5.6 uM.

Protocol
Cell Experiment
Cell lines HeLa, HCT116, HT29, LOVO, DU145, and NHDF cells
Preparation method Seeding cells (5 ×103 to 1.5 ×104 per cm2) in 24-well plate. 24 hours later, treating plates with PHA-680632 and incubating for 72 hours. At the end of incubation time, detaching cells from each plate and using a cell counter to count . Calculating IC50s using percentage of growth versus untreated cont
Concentrations 0.001-1 μM, dissolved in DMSO as 10 mM stock solution
Incubation time 72 hours
Animal Experiment
Animal models Mice (female athymic nude) xenografts models of p53−/− HCT116 cells
Formulation Dissolved in 20% Tween-80 in 5% glucose solution
Dosages 40 mg/kg
Administration Intraperitoneal (i.p.) injection twice a day
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 501.62
Formula C28H35N7O2
CAS Number 398493-79-3
Purity >98%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

[1] Laura Mazzera, et al. Functional interplay between NF-κB-inducing kinase and c-Abl kinases limits response to Aurora inhibitors in multiple myeloma

[2] Alessio Polacchini, et al. Combined cisplatin and aurora inhibitor treatment increase neuroblastoma cell death but surviving cells overproduce BDNF

[3] Laura Mazzera, et al. Aurora and IKK kinases cooperatively interact to protect multiple myeloma cells from Apo2L/TRAIL

[4] V Ratushny, et al. Dual inhibition of SRC and Aurora kinases induces postmitotic attachment defects and cell death

[5] Chiara Soncini, et al. PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity

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  Catalog
Abmole Inhibitor Catalog




Keywords: PHA-680632 supplier, Aurora Kinase, inhibitors

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