Cat. No.: HY-70044

GSK-1070916

(Synonyms: GSK-1070916A)

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

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Pureté: 99.54%
CAS No.: 942918-07-2
Formule: C₃₀H₃₃N₇O
Masse moléculaire:507.63

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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GSK-1070916 Chemical Structure

CAS No.: 942918-07-2

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- Cellular Effect
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Description

GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with K_is 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)

Voir tous les produits spécifiques à Isoform Aurora Kinase :

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	EC₅₀	57 nM Compound: GSK 1070916	Antiproliferative activity against human 786-0 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human 786-0 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
A2780	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human A2780 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human A2780 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
A375P	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human A375P cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human A375P cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
A498	EC₅₀	33 nM Compound: GSK 1070916	Antiproliferative activity against human A498 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human A498 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
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]
A549	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human A549 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human A549 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
A549	EC₅₀	7 nM Compound: GSK-1070916	Cytotoxicity against human A549 cells in presence of 10% human serum Cytotoxicity against human A549 cells in presence of 10% human serum	[PMID: 20335034]
ARH-77	EC₅₀	15 nM Compound: GSK 1070916	Antiproliferative activity against human ARH-77 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human ARH-77 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
ASPC1	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human ASPC1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
BC-3	EC₅₀	27 nM Compound: GSK 1070916	Antiproliferative activity against human BC-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human BC-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
BV-173	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human BV-173 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human BV-173 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
BXPC-3	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CA46	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human CA46 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CA46 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CCRF-CEM	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human CCRF-CEM cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CCRF-CEM cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CCRF-HSB-2	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human HSB-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HSB-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CCRF-SB	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human CCRF-SB cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CCRF-SB cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CESS	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human CESS cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CESS cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CMK	EC₅₀	27 nM Compound: GSK 1070916	Antiproliferative activity against human CMK cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CMK cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
COLO 201	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human COLO201 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human COLO201 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
COLO 205	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human COLO 205 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human COLO 205 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
COLO 320DM	EC₅₀	96 nM Compound: GSK 1070916	Antiproliferative activity against human COLO 320DM cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human COLO 320DM cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
COLO-320-HSR	EC₅₀	92 nM Compound: GSK 1070916	Antiproliferative activity against human COLO 320HSR cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human COLO 320HSR cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CRO-AP2	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human CRO-AP2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CRO-AP2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
CTV-1	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human CTV-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human CTV-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Daudi	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human Daudi cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Daudi cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
DB	EC₅₀	11 nM Compound: GSK 1070916	Antiproliferative activity against human DB cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human DB cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
DG-75	EC₅₀	18 nM Compound: GSK 1070916	Antiproliferative activity against human DG-75 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human DG-75 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
DLD-1	EC₅₀	28 nM Compound: GSK 1070916	Antiproliferative activity against human DLD-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human DLD-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
DOHH-2	EC₅₀	14 nM Compound: GSK 1070916	Antiproliferative activity against human DOHH-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human DOHH-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
DU-145	EC₅₀	15 nM Compound: GSK 1070916	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human DU-145 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
EB2	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human EB2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human EB2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
EB-3	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human EB-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human EB-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
EM-2	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human EM-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human EM-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Farage	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human Farage cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Farage cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
GA-10	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human GA-10 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human GA-10 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
GDM-1	EC₅₀	21 nM Compound: GSK 1070916	Antiproliferative activity against human GDM-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human GDM-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HCT-116	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HCT-8	EC₅₀	38 nM Compound: GSK 1070916	Antiproliferative activity against human HCT-8 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HCT-8 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HD-MY-Z	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human HD-MY-Z cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HD-MY-Z cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HEL 92.1.7	EC₅₀	60 nM Compound: GSK 1070916	Antiproliferative activity against human HEL 92.1.7 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HEL 92.1.7 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HeLa	EC₅₀	13 nM Compound: GSK 1070916	Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Hep 3B2	EC₅₀	12 nM Compound: GSK 1070916	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HH	EC₅₀	18 nM Compound: GSK 1070916	Antiproliferative activity against human HH cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HH cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HL-60	EC₅₀	10 nM Compound: GSK 1070916	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HN5	EC₅₀	10 nM Compound: GSK 1070916	Antiproliferative activity against human HN5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HN5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HT	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human HT cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HT cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HT-29	EC₅₀	10 nM Compound: GSK 1070916	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HuT78	EC₅₀	14 nM Compound: GSK 1070916	Antiproliferative activity against human HuT78 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human HuT78 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
HUVEC	EC₅₀	3900 nM Compound: GSK 1070916	Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 6 days by cell titer glo assay Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 6 days by cell titer glo assay	[PMID: 19567821]
JIYOYE	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human JIYOYE cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human JIYOYE cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
JM1	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human JM1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human JM1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
J-RT3-T3-5	EC₅₀	9 nM Compound: GSK 1070916	Antiproliferative activity against human J-RT3-T3-5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human J-RT3-T3-5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Jurkat	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
JVM-3	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human JVM-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human JVM-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
K562	EC₅₀	13 nM Compound: GSK 1070916	Antiproliferative activity against human K562 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human K562 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
KCL-22	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human KCL-22 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human KCL-22 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
KG-1	EC₅₀	32 nM Compound: GSK 1070916	Antiproliferative activity against human KG-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human KG-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
L-428	EC₅₀	31 nM Compound: GSK 1070916	Antiproliferative activity against human L-428 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human L-428 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
LNCaP	EC₅₀	12 nM Compound: GSK 1070916	Antiproliferative activity against human LNCaP cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human LNCaP cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
LoVo	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human LoVo cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human LoVo cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MC116	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human MC116 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MC116 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MC-CAR	EC₅₀	9 nM Compound: GSK 1070916	Antiproliferative activity against human MC-CAR cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MC-CAR cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MCF7	EC₅₀	13 nM Compound: GSK 1070916	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MDA-MB-231	EC₅₀	11 nM Compound: GSK 1070916	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MDA-MB-453	EC₅₀	6 nM Compound: GSK 1070916	Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MDA-MB-468	EC₅₀	12 nM Compound: GSK 1070916	Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MEG-01	EC₅₀	44 nM Compound: GSK 1070916	Antiproliferative activity against human MEG-01 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MEG-01 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MHH-PREB-1	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human MHH-PREB-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MHH-PREB-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MIA PaCa-2	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human Mia PaCa cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Mia PaCa cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
ML-2	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human ML-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human ML-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MOLT-16	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human MOLT-16 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MOLT-16 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MOLT-3	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human MOLT-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MOLT-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MOLT-4	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MV4-11	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
MX1	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human MX1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human MX1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NALM-6	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human NALM-6 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NALM-6 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NAMALVA	EC₅₀	6 nM Compound: GSK 1070916	Antiproliferative activity against human NAMALWA cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NAMALWA cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NB-4	EC₅₀	11 nM Compound: GSK 1070916	Antiproliferative activity against human NB4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NB4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NC-37	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human NC-37 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NC-37 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NCI-H1155	EC₅₀	40 nM Compound: GSK 1070916	Antiproliferative activity against human NCI-H1155 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NCI-H1155 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NCI-H1299	EC₅₀	23 nM Compound: GSK 1070916	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NCI-H157	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human NCI-H157 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NCI-H157 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NCI-H358	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human NCI-H358 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NCI-H358 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NCI-H460	EC₅₀	14 nM Compound: GSK 1070916	Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NCI-H630	EC₅₀	127 nM Compound: GSK 1070916	Antiproliferative activity against human NCI-H630 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NCI-H630 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NOMO-1	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human NOMO-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NOMO-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
NU-DUL-1	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human NU-DUL-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human NU-DUL-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
OCI-AML2	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human OCI-AML2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human OCI-AML2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
OCI-AML-3	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human OCI-AML-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human OCI-AML-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
OCI-LY19	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human OCILY19 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human OCILY19 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
OVCAR-3	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
OVCAR-4	EC₅₀	11 nM Compound: GSK 1070916	Antiproliferative activity against human OVCAR-4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human OVCAR-4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
OVCAR-8	EC₅₀	30 nM Compound: GSK 1070916	Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human OVCAR-8 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
P3HR-1	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human P3HR-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human P3HR-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
PANC-1	EC₅₀	13 nM Compound: GSK 1070916	Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
PC-3	EC₅₀	11 nM Compound: GSK 1070916	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Pfeiffer	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human Pfeiffer cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Pfeiffer cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Raji	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human Raji cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Raji cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
RCK8	EC₅₀	38 nM Compound: GSK 1070916	Antiproliferative activity against human RCK8 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human RCK8 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Rec1	EC₅₀	77 nM Compound: GSK 1070916	Antiproliferative activity against human REC1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human REC1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
RKO	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human RKO cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human RKO cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
RL	EC₅₀	10 nM Compound: GSK 1070916	Antiproliferative activity against human RL cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human RL cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
RPMI-6666	EC₅₀	10 nM Compound: GSK 1070916	Antiproliferative activity against human RPMI-6666 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human RPMI-6666 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
RPMI-8226	EC₅₀	111 nM Compound: GSK 1070916	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SEM	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human SEM cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SEM cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SK-BR-3	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SK-MEL-2	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human SK-MEL-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SK-MEL-2 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SK-MEL-28	EC₅₀	7 nM Compound: GSK 1070916	Antiproliferative activity against human SK-MEL-28 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SK-MEL-28 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SK-MEL-5	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human SK-MEL-5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SK-MEL-5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SK-OV-3	EC₅₀	12 nM Compound: GSK 1070916	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SR	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human SR cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SR cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
ST486	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human ST486 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human ST486 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SUD4	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human SU-DHL-4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SU-DHL-4 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SU-DHL10	EC₅₀	15 nM Compound: GSK 1070916	Antiproliferative activity against human SU-DHL-10 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SU-DHL-10 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SU-DHL-16	EC₅₀	4 nM Compound: GSK 1070916	Antiproliferative activity against human SU-DHL-16 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SU-DHL-16 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SU-DHL-5	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human SU-DHL-5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SU-DHL-5 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SU-DHL-6	EC₅₀	6 nM Compound: GSK 1070916	Antiproliferative activity against human SU-DHL-6 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SU-DHL-6 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SUP-B15	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human SUP-B15 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SUP-B15 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SW 954	EC₅₀	11 nM Compound: GSK 1070916	Antiproliferative activity against human SW 954 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SW 954 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SW1417	EC₅₀	19 nM Compound: GSK 1070916	Antiproliferative activity against human SW1417 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SW1417 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SW48	EC₅₀	2 nM Compound: GSK 1070916	Antiproliferative activity against human SW48 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SW48 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SW480	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human SW480 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SW480 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
SW-620	EC₅₀	8 nM Compound: GSK 1070916	Antiproliferative activity against human SW620 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human SW620 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
T47D	EC₅₀	13 nM Compound: GSK 1070916	Antiproliferative activity against human T47D cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human T47D cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
THP-1	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
Toledo	EC₅₀	15 nM Compound: GSK 1070916	Antiproliferative activity against human Toledo cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human Toledo cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
U-266	EC₅₀	422 nM Compound: GSK 1070916	Antiproliferative activity against human U266B1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human U266B1 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
U2OS	EC₅₀	34 nM Compound: GSK 1070916	Antiproliferative activity against human U2OS cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human U2OS cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
U-937	EC₅₀	5 nM Compound: GSK 1070916	Antiproliferative activity against human U-937 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human U-937 cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]
WiDr	EC₅₀	3 nM Compound: GSK 1070916	Antiproliferative activity against human WiDr cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay Antiproliferative activity against human WiDr cells assessed as inhibition of cell viability measured for 6 to 7 days by cell titer glo assay	[PMID: 19567821]

In Vitro

GSK-1070916 potently inhibits Aurora B/INCENP and Aurora C/INCENP kinases with K_is of 0.38±0.29 and 1.45±0.35 nM, respectively, but is less potent against Aurora A/ TPX2 with a K_i 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.

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 942918-07-2
Appearance Solid
Masse moléculaire 507.63
Formule C₃₀H₃₃N₇O
Color 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
Synonyms

GSK-1070916A
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (5)

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Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Mol Cancer Ther

AKT Inhibition Sensitizes to Polo-Like Kinase 1 Inhibitor Onvansertib in Prostate Cancer. [Abstract]

2024 Oct 1;23(10):1404-1417. PMID: 38894678
JCI Insight

Cell cycle inhibitors activate the hypoxia-induced DDX41/STING pathway to mediate antitumor immune response in liver cancer. [Abstract]

2024 Nov 22;9(22):e170532. PMID: 39388278
bioRxiv

Nucleosome stability safeguards cell identity, stress resilience and healthy aging. [Abstract]

2025 Sep 18:2025.09.17.676776. PMID: 41000743
J Biomol Screen

Differential determinants of cancer cell insensitivity to antimitotic drugs discriminated by a one-step cell imaging assay. [Abstract]

2013 Oct;18(9):1062-71. PMID: 23788527

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1 mg/mL (1.97 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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).

Working solution concentration: 0.22 mg/mL

Protocole

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].

MedChemExpress (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].

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Adams ND, et al. Discovery of GSK-1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001. [Content Brief]

[2]. Hardwicke MA, et al. GSK-1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models. Mol Cancer Ther. 2009 Jul;8(7):1808-17. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

GSK-1070916

5 Cited Publications

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GSK-1070916

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Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK-1070916

Voir tous les produits spécifiques à Isoform Aurora Kinase

Activité biologique

Chemical Information

Publications (5)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GSK-1070916

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK-1070916

Voir tous les produits spécifiques à Isoform Aurora Kinase

Activité biologique

Chemical Information

Publications (5)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GSK-1070916 Related Classifications

HY-70044 Related Classifications