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PHA-680632

Catalog No. T6338 CAS 398493-79-3

Synonyms: PHA 680632, PHA680632

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.

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PHA-680632, CAS 398493-79-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 147.00
50 mg	In stock	$ 255.00
100 mg	In stock	$ 427.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 99.03%

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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:27 nM, Aurora B:135 nM, Aurora C:120 nM
In vitro	PHA-680632 potently inhibits all three Aurora kinases (A, B, and C) with IC50 values of 27, 135, and 120 nM, respectively. PHA-680632 is selective for Aurora kinases, with 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, VEGFR2, and VEGFR3, and with IC50 higher than 10 μM for another 22 kinases. PHA-680632 shows potent anti-proliferative effects in a wide range of cell types with IC50 values of 0.06–7.15 μM, including HeLa, HCT116, HT29, LOVO, DU145, and NHDF cells. PHA-680632 (0.5 μM) causes polyploidy in tumor cells. The mechanism of action of PHA-680632 is in agreement with inhibition of Aurora kinases. [1] PHA680632 in association with radiation leads to additive effects in cancer cells, especially in the p53-deficient cells. Combined ionising radiation (IR) and treatment of PHA680632 (100–400 nM) prior to IR leads to an enhancement of radiation-induced Annexin V positive cells, micronuclei formation, and Brca1 foci formation only in HCT116 cells with deficient p53, other than the p53 wild-type counterparts. [2]
In vivo	HA-680632 (15–60 mg/kg) inhibits tumor growth in mice xenografts models of HL60, A2780, and HCT116 cells, by reducing tumor cell proliferation and increasing apoptosis. PHA-680632 (45 mg/kg) suppresses growth of activated ras-driven mammary tumors in mouse mammary tumor virus v-Ha-ras transgenic mice and results in complete tumor stabilization and partial regression. [1]
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)

Synonyms	PHA 680632, PHA680632
Molecular Weight	501.62
Formula	C28H35N7O2
CAS No.	398493-79-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (185.4 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

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 compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Osteogenesis Compound Library Anti-Lung Cancer Compound Library Bioactive Compounds Library Max Cell Cycle Compound Library Cytokine Inhibitor Library Anti-Fibrosis Compound Library

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Keywords

PHA-680632 398493-79-3 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic Tyrosine Kinase/Adaptors PLK FGFR Aurora Kinase PHA 680632 Inhibitor inhibit PHA680632 inhibitor

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