A potent inhibitor of Aurora B and C (Kis = 0.38 and 1.5 nM

GSK1070916 – 25 mg

Brand:
Cayman
CAS:
942918-07-2
Storage:
-20
UN-No:
Non-Hazardous - /

GSK1070916 is a potent and ATP-competitive inhibitor of Aurora kinases B and C (Kis = 0.38 and 1.5 nM, respectively).{43055} It is >250-fold selective for Aurora B and C over Aurora A. GSK1070916 inhibits proliferation of A549 lung cancer cells in vitro (EC50 = 7 nM). It also inhibits proliferation in a panel of 100 tumor cell lines (EC50s = via induction of polyploidy and apoptosis.{43056} In vivo, GSK1070916 inhibits histone H3 phosphorylation in a COLO 205 mouse xenograft model and induces tumor regression in an HL-60 mouse xenograft model.{43055} It also reduces tumor growth in 10 mouse xenograft models, including models of breast, colon, and lung carcinomas as well as leukemias.{43056}  

 

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SKU: 22953 - 25 mg Category:

Description

A potent inhibitor of Aurora B and C (Kis = 0.38 and 1.5 nM, respectively); >250-fold selective for Aurora B and C over Aurora A; inhibits proliferation of A549 lung cancer cells in vitro (EC50 = 7 nM); inhibits proliferation in a panel of 100 tumor cell lines (EC50s = <10 nM); inhibits histone H3 phosphorylation in a COLO 205 mouse xenograft model and induces tumor regression in an HL-60 mouse xenograft model; reduces tumor growth in 10 mouse xenograft models

Formal name: 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-urea

Synonyms: 

Molecular weight: 507.6

CAS: 942918-07-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Aurora||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Aurora Signaling

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