GSK-1070916


CAS No. : 942918-07-2

(Synonyms: GSK-1070916A)

942918-07-2
Price and Availability of CAS No. : 942918-07-2
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5mg $119 In-stock
10mg $198 In-stock
50mg $528 In-stock
100mg $924 In-stock
200mg $1584 In-stock
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Cat. No. : HY-70044
M.Wt: 507.63
Formula: C30H33N7O
Purity: >98 %
Solubility: DMSO : 16.67 mg/mL (32.84 mM; ultrasonic and warming and heat to 60°C)
Introduction of 942918-07-2 :

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].

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