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

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
5 mg USD 50 In-stock
10 mg USD 90 In-stock
25 mg USD 180 In-stock
50 mg USD 310 In-stock
100 mg USD 520 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

PHA-680632 Related Antibodies

Top Publications Citing Use of Products

View All Aurora Kinase Isoform Specific Products:

View All Isoforms
Aurora Kinase Aurora A Aurora B Aurora C

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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)

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
0.045 μM
Compound: 31, PHA-680632
Antiproliferative activity against human HCT116 cells assessed as BrdU incorporation after 72 hrs
Antiproliferative activity against human HCT116 cells assessed as BrdU incorporation after 72 hrs
[PMID: 19320489]
MOLT-4 EC50
0.22 μM
Compound: 2, PHA-680632
Cytotoxicity against human MOLT4 cells assessed as inhibition of cell growth after 4 days by Cell Titer Blue end-point assay
Cytotoxicity against human MOLT4 cells assessed as inhibition of cell growth after 4 days by Cell Titer Blue end-point assay
[PMID: 22889561]
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].

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

PHA-680632 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

501.62

Formula

C28H35N7O2
CAS No.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (59.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.07%

SDS (393 KB)

COA (251 KB) HNMR (299 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9935 mL 9.9677 mL 19.9354 mL 49.8385 mL
5 mM 0.3987 mL 1.9935 mL 3.9871 mL 9.9677 mL
10 mM 0.1994 mL 0.9968 mL 1.9935 mL 4.9839 mL
15 mM 0.1329 mL 0.6645 mL 1.3290 mL 3.3226 mL
20 mM 0.0997 mL 0.4984 mL 0.9968 mL 2.4919 mL
25 mM 0.0797 mL 0.3987 mL 0.7974 mL 1.9935 mL
30 mM 0.0665 mL 0.3323 mL 0.6645 mL 1.6613 mL
40 mM 0.0498 mL 0.2492 mL 0.4984 mL 1.2460 mL
50 mM 0.0399 mL 0.1994 mL 0.3987 mL 0.9968 mL
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PHA-680632 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PHA-680632398493-79-3PHA680632PHA 680632Aurora KinaseInhibitorinhibitorinhibit

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