1. Cell Cycle/DNA Damage
    Epigenetics
  2. Aurora Kinase

GSK-1070916 (Synonyms: GSK-1070916A)

Cat. No.: HY-70044 Purity: 99.55%
Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 121 In-stock
5 mg USD 108 In-stock
10 mg USD 180 In-stock
50 mg USD 480 In-stock
100 mg USD 840 In-stock
200 mg USD 1440 In-stock
500 mg   Get quote  
1 g   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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

Ki: 0.38 nM (Aurora B), 1.5 nM (Aurora C)[1]

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].

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].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume 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
10 mM 0.1970 mL 0.9850 mL 1.9699 mL
Please refer to the solubility information to select the appropriate solvent.
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]

GSK-1070916 is prepared in 2% Cremophor EL, 2% N,N-dimethylacetamide, and 96% acidified water (pH 5.0)[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
Molecular Weight

507.63

Formula

C₃₀H₃₃N₇O

CAS No.

942918-07-2

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 26.5 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.55%

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Product Name:
GSK-1070916
Cat. No.:
HY-70044
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