2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Aurora Kinase Apoptosis
  4. GSK-1070916

GSK-1070916  (Synonyms: GSK-1070916A)

Cat. No.: HY-70044 Purity: 98.99%
SDS COA Handling Instructions

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GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.

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

GSK-1070916 Chemical Structure

GSK-1070916 Chemical Structure

CAS No. : 942918-07-2

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Customer Review

Based on 5 publication(s) in Google Scholar

GSK-1070916 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

GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.

IC50 & Target[1]

Aurora B

0.38 nM (Ki)

Aurora C

1.5 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
A549 EC50
7 nM
Compound: 17k, GSK-1070916
Antiproliferative activity against human A549 cells after 6 to 7 days by celltiter-glo luminescence assay in absence of 70% human serum albumin
Antiproliferative activity against human A549 cells after 6 to 7 days by celltiter-glo luminescence assay in absence of 70% human serum albumin
[PMID: 20420387]
In Vitro

GSK-1070916 potently inhibits Aurora B/INCENP and Aurora C/INCENP kinases with Kis of 0.38±0.29 and 1.45±0.35 nM, respectively, but is less potent against Aurora A/ TPX2 with a Ki of 492±61 nM. GSK-1070916 also inhibits FLT1, TIE2, SIK, FLT4, and FGFR1 with IC50 values of 42, 59, 70, 74, and 78 nM, respectively. Treatment of A549 human lung cancer cells with GSK-1070916 results in a potent antiproliferative effect (EC50=7 nM)[1]. GSK-1070916 inhibits a panel of tumor cell lines and is shown o inhibits the phosphorylation of HH3- S10 in all cell lines with average EC50 values ranging from 8 to 118 nM[2].

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

GSK-1070916 Related Antibodies
In Vivo

In nude mice implanted with human colon tumor (HCT116) xenografts, a single dose of GSK-1070916 administered i.p. inhibits HH3-S10 phosphorylation in a dose-dependent manner. Repeated i.p. administration of GSK-1070916 produces complete or partial antitumor activity in 4 of 8 tumor types [lung, A549; colon, HCT116; acute myelogenous leukemia (AML), HL60; and chronic myelogenous leukemia, K562], stable disease in 3 of 8 (colon, Colo205; lung, H460; and breast, MCF-7), and tumor growth delay in 1 of 8 tumor types (colon, SW620). Daily administration of GSK-1070916 is generally well-tolerated[2].

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

507.63

Formula

C30H33N7O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1=CC=C(C2=NN(C=C2C3=C4C(NC(C5=CC=CC(CN(C)C)=C5)=C4)=NC=C3)CC)C=C1)N(C)C
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 : 16.67 mg/mL (32.84 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9699 mL 9.8497 mL 19.6994 mL
5 mM 0.3940 mL 1.9699 mL 3.9399 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.

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  • 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: ≥ 1.67 mg/mL (3.29 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: ≥ 1.67 mg/mL (3.29 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: 99.55%

SDS (393 KB)

COA (249 KB) HNMR (185 KB) LCMS (469 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[2]

A panel of tumor cell lines are plated in 96-well plates in the recommended growth media and incubated at 37°C in 5% CO2 overnight. The following day, the cells are treated with serial dilutions of GSK-1070916. At this time, one set of cells is treated with CellTiter-Glo for a time equal to 0 (T=0) measurement. Following a 6- to 7-d incubation with compound, cell proliferation is measured using the CellTiter-Glo reagent[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice: Tumors are initiated by injection of tumor cell suspensions (A549, SW620, HCT116, H460, MCF-7, HL60, K562) or tumor fragments (Colo205) s.c. into nude (A549, SW620, HCT116, H460, MCF-7, HL60, and Colo205) or severe combined immunodeficient (SCID; K562) mice. When the tumors reach a volume of 80 to 200 mm3, the mice are randomized into groups of 5 to 10 mice per group. GSK-1070916 is administered at 25, 50, or 100 mg/kg once daily for 5 consecutive days-on, 2d-off, schedule for two (Colo205 and HL60) or three (A549, SW620, HCT116, H460, MCF-7, K562) cycles. Tumors are measured twice weekly[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 1.9699 mL 9.8497 mL 19.6994 mL 49.2485 mL
5 mM 0.3940 mL 1.9699 mL 3.9399 mL 9.8497 mL
10 mM 0.1970 mL 0.9850 mL 1.9699 mL 4.9248 mL
15 mM 0.1313 mL 0.6566 mL 1.3133 mL 3.2832 mL
20 mM 0.0985 mL 0.4925 mL 0.9850 mL 2.4624 mL
25 mM 0.0788 mL 0.3940 mL 0.7880 mL 1.9699 mL
30 mM 0.0657 mL 0.3283 mL 0.6566 mL 1.6416 mL
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GSK-1070916 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:

GSK-1070916942918-07-2GSK-1070916AGSK1070916GSK 1070916Aurora KinaseApoptosisInhibitorinhibitorinhibit

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