Free shipping on all orders over $ 500

PHA-680632

Cat. No. M3552

PHA-680632 Structure
Size Price Availability
5mg USD 165 Out of stock
10mg USD 300 Out of stock
50mg USD 920 Out of stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • 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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 501.62
Formula C28H35N7O2
CAS Number 398493-79-3
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
Related Aurora Kinase Products
SNS-314

SNS-314 is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively.

GSK1070916

GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex.

MK-5108

MK-5108 (VX-689) is a highly selective Aurora A inhibitor with IC50 of 0.064 nM and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity.

PF-03814735

PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1.

MK-8745

MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PHA-680632 supplier, Aurora Kinase, inhibitors

Contact Us
  • Tel: +1-800-660-8580
  • Email: sales@abmole.com
  • Tel: +32 (0)2 738 09 61
  • Email: eu.order@abmole.com

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.