GSK-1070916

SKU: orb1223566

Description

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.

Images & Validation

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Key Properties

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CAS Number	942918-07-2
MW	507.6293
Purity	>98% (HPLC)
Formula	C₃₀H₃₃N₇O
SMILES	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
Target	Aurora Kinase
Solubility	DMSO: ≥ 26.5 mg/mL

Bioactivity

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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.

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). 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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GSK1070916 | GSK 1070916

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Aurora Kinase

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GSK-1070916 (orb1223566)

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Purity:	99.73%
CAS Number:	942918-07-2
MW:	507.63
Formula:	C₃₀H₃₃N₇O

GSK-1070916

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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GSK-1070916 (orb1223566)

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