GSK-1070916

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Aurora B 和 C 的有效、选择性和 ATP 竞争性抑制剂，Ki 分别为 0.38 nM 和 1.5 nM。

A potent, selective and ATP-competitive inhibitor of Aurora B and C with Ki of 0.38 nM and 1.5 nM, respectively; displays >250-fold selectivity over Aurora A; shows potent antiproliferative effect (EC50=7 nM) in A549 human lung cancer cells; causes inhibition of histone H3 phosphorylation at serine 10 in human colon cancer (Colo205) and tumor regression in human leukemia (HL-60) in mice.Ovarian Cancer Phase 2 Clinical.

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). 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.

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.

GSK1070916 | GSK 1070916

Cell Cycle/DNA Damage

Aurora Kinase

SIK| Aurora B-INCENP| Aurora C-INCENP| FLT1| Tie-2

Cancer

Ovarian Cancer

942918-07-2

507.6293

C30H33N7O

>98% (HPLC)

DMSO: ≥ 26.5 mg/mL

O=C(NC1=CC=C(C2=NN(CC)C=C2C3=C4C(NC(C5=CC=CC(CN(C)C)=C5)=C4)=NC=C3)C=C1)N(C)C

Urea, N'-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethyl-1H-pyrazol-3-yl]phenyl]-N,N-dimethyl-

(-20℃)

With Ice Pack

≥ 2 years