1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase
  3. PHA-680632

PHA-680632 

Cat. No.: HY-10178 Purity: 98.48%
Handling Instructions

PHA-680632 is an aurora kinase inhibitor with IC50s of 27, 135 and 120 nM for aurora A, B and C, respectively.

For research use only. We do not sell to patients.

PHA-680632 Chemical Structure

PHA-680632 Chemical Structure

CAS No. : 398493-79-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 146 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1008 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1524 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Protocol

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Description

PHA-680632 is an aurora kinase inhibitor with IC50s of 27, 135 and 120 nM for aurora A, B and C, respectively.

IC50 & Target[1]

Aurora A

27 nM (IC50)

Aurora B

135 nM (IC50)

Aurora C

120 nM (IC50)

In Vitro

PHA-680632 shows 30- to 200-fold higher IC50s of FLT3, LCK, PLK1, STLK2, VEGFR2, and VEGFR3 compared with Aurora A. PHA-680632 has potent antiproliferative activity in a wide range of cell types. The IC50s are 0.32, 0.41, 0.06, 1.17, 0.56, 0.62, 0.29, 0.11, 1.56, 0.62, 0.07, 0.13, 0.41 μM for C33A, HeLa, HCT116, HT29, LOVO, A549, MCF7, A2780, U2OS, DU145, U937, HL60, NHDF. PHA-680632 can cause polyploidy in tumor cells. PHA-680632 cell treatment induces phenotypes similar to Aurora A or B depletion[1]. PHA680632, inhibits colony formation in different cancer cell lines and induced polyploidy. Aurora-A inhibition by PHA680632 enhances radiation response in cancer cells, especially in p53-deficient cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PHA-680632 suppresses tumor growth in animal models. PHA-680632 treatment at 45 mg/kg dose results in 85% of TGI without signs of toxicity in the HL60 human acute myelogenous leukemia xenograft model. PHA-680632 treatment at 60 mg/kg i.v. b.i.d. for 5 days results in 78% of TGI without signs of toxicity in the A2780 human ovarian carcinoma model[1]. PHA680632 in association with radiation leads to an additive effect in cancer cells, especially in the p53-deficient cells, but does not act as a radiosensitiser[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

501.62

Formula

C₂₈H₃₅N₇O₂

CAS No.

398493-79-3

SMILES

O=C(N1CC2=C(NN=C2NC(C3=CC=C(N4CCN(C)CC4)C=C3)=O)C1)NC5=C(C=CC=C5CC)CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (59.81 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9935 mL 9.9677 mL 19.9354 mL
5 mM 0.3987 mL 1.9935 mL 3.9871 mL
10 mM 0.1994 mL 0.9968 mL 1.9935 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Inhibition of kinase activity by PHA-680632 is assessed using a scintillation proximity assay format. In this assay, 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 Auroratide1 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 and 29 additional kinases belonging to our Kinase Selectivity Screening panel is evaluated and the relevant IC50s are determined[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Cells are seeded at different densities ranging from 5,000 to 15,000 cm2 in 24-well plate with the appropriate complete medium. After 24 hours, plates are treated with PHA-680632 and incubated for 72 hours at 37°C in 5% CO2 atmosphere. 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 control[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice: Tumour xenograft mice are randomly allocated into four groups (six mice per group): A, control; B, IR alone, 8 Gy in 1 day; C, PHA-680632 alone, 40 mg/kg, b.i.d., for 4 days; D, same dose of PHA-680632 combined with IR (24 h after the first administration of PHA680632, similar schedule as IR alone) for 4 days. Drug or vehicle control (same volume of 20% Tween-80 in 5% glucose solution) is administered intraperitoneally (i.p.). The tumour size is measured twice a week using an electronic caliper. Follow-up of individual mice is conducted. The tumour volume is estimated from 2D tumour measurements[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 98.48%

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Keywords:

PHA-680632PHA680632PHA 680632Aurora KinaseInhibitorinhibitorinhibit

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PHA-680632
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