GW843682X [660868-91-7]
Cat# HY-11003-5mg
Size : 5mg
Brand : MedChemExpress
GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ∼30 other kinases.
For research use only. We do not sell to patients.
GW843682X Chemical Structure
CAS No. : 660868-91-7
This product is a controlled substance and not for sale in your territory.
Based on 5 publication(s) in Google Scholar
Description |
GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ∼30 other kinases. |
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IC50 & Target[1] |
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In Vitro |
GW843682X (compound 1) is effective on inhibition of growth of tumor cells, with IC50s of 0.41, 0.57, 0.11, 0.38, and 0.70 μM for A549, BT474, HeLa, H460 and HCT116 cell lines. GW843682X dose-dependently inhibits PLK1 phosphorylation of Ser15-p53, with an IC50 of 0.14 μM. GW843682X (3 μM) causes a strong G2-M arres in HDF cells and H460 cells after treatment for 24, 48, and 72 h. GW843682X (5 μM) leads to apoptosis in H460 cells instead of HDF cells[1]. GW843682X inhibits proliferation of U937 cells with an EC50 of 120 nM. GW843682X (500 nM) in combination with 5 µM VP-16 suppresses 50% of entry into mitosis in U937 cells[2]. GW843682X (0.06-1 μM) has inhibitory activities against proliferation of acute leukemia cells, and potentiates the anti-proliferative activity of vincristine. Moreover, GW843682X (0.1-1 μM) induces apoptosis of leukemia cells in a dose- and time-dependent manner. GW843682X (0.5-1 μM) dephosphorylates Bcl-xl in leukemia cells[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Molecular Weight |
477.46 |
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Formula |
C22H18F3N3O4S |
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CAS No. |
660868-91-7 |
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Appearance |
Solid |
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Color |
Light yellow to yellow |
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SMILES |
O=C(C1=C(OCC2=CC=CC=C2C(F)(F)F)C=C(N3C4=CC(OC)=C(OC)C=C4N=C3)S1)N |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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Solvent & Solubility |
In Vitro:
DMSO : 33.33 mg/mL (69.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume 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
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.
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Purity & Documentation |
Purity: 99.75% |
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References |
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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 |
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DMSO | 1 mM | 2.0944 mL | 10.4721 mL | 20.9442 mL | 52.3604 mL |
5 mM | 0.4189 mL | 2.0944 mL | 4.1888 mL | 10.4721 mL | |
10 mM | 0.2094 mL | 1.0472 mL | 2.0944 mL | 5.2360 mL | |
15 mM | 0.1396 mL | 0.6981 mL | 1.3963 mL | 3.4907 mL | |
20 mM | 0.1047 mL | 0.5236 mL | 1.0472 mL | 2.6180 mL | |
25 mM | 0.0838 mL | 0.4189 mL | 0.8378 mL | 2.0944 mL | |
30 mM | 0.0698 mL | 0.3491 mL | 0.6981 mL | 1.7453 mL | |
40 mM | 0.0524 mL | 0.2618 mL | 0.5236 mL | 1.3090 mL | |
50 mM | 0.0419 mL | 0.2094 mL | 0.4189 mL | 1.0472 mL | |
60 mM | 0.0349 mL | 0.1745 mL | 0.3491 mL | 0.8727 mL |