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Angiogenesis FGFR PHA680632

PHA680632

Catalog No. T6338   CAS 398493-79-3
Synonyms: PHA-680632, PHA 680632

PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3.

PHA680632, CAS 398493-79-3
Pack Size Availability Price/USD Quantity
2 mg In stock 73.00
5 mg In stock 129.00
10 mg In stock 233.00
25 mg In stock 455.00
50 mg In stock 748.00
100 mg In stock 1369.00
1 mL * 10 mM (in DMSO) In stock 145.00
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Purity 98.0%
Biological Description
Chemical Properties
Storage & Solubility Information
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Description PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3.
Targets&IC50 Aurora A : ic50 27nM,   Aurora B : ic50 135nM,   Aurora C : ic50 120nM,   FGFR1 : ic50 390nM,   PLK1 : ic50 780nM,  
Kinase Assay Aurora Kinase Inhibition Assay: Inhibition of kinase activity by PHA-680632 is assessed using a scintillation proximity assay format. The biotinylated substrate is transphosphorylated by the kinase in presence of ATP traced with γ33-ATP. The phosphorylated substrate is then captured using streptavidin-coated scintillation proximity assay beads and the extent of phosphorylation is evaluated by β-counter after a 4-hour rest for the floatation of the beads on a dense 5 M CsCl solution. In particular, a peptide derived from the Chocktide sequence (LRRWSLGL) is used as substrate for Aurora A, whereas the optimized peptide Auroratide is employed for Aurora B and C. The assay is run in a robotized format on 96-well plates. The potency of the compound toward Aurora kinases is evaluated and IC50 values are determined.
Cell Research
Cells (5 × 103 to 1.5 × 104 per cm2) are seeded in 24-well plate. After 24 hours, plates are treated with PHA-680632 and incubated for 72 hours. At the end of incubation time, cells are detached from each plate and counted using a cell counter. IC50s are calculated using percentage of growth versus untreated cont(Only for Reference)
Cell lines: HeLa, HCT116, HT29, LOVO, DU145, and NHDF cells
Animal Research
Animal Model: Mice (feathymic nude) xenografts models of p53−/− HCT116 cells
Synonyms PHA-680632 , PHA 680632
Purity 98.0%
Molecular Weight 501.62
Formula C28H35N7O2
CAS No. 398493-79-3

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 93 mg/mL (185.4 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

10% Tween 80: 30 mg/mL

Citations

References and Literature
1. Soncini C, et al. Clin Cancer Res, 2006, 12(13), 4080-4089. 2. Tao Y, et al. Br J Cancer, 2007, 97(12), 1664-1672.

Related Products

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ON-01910 SP-146 Sorafenib tosylate KW2449 DGY-06-116 PRN1371 BO-264 Aurora Kinase Inhibitor III

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