A potent pan-Aurora kinase inhibitor that favors Aurora A (Ki = 0.6 nM) over Aurora B (Ki = 18 nM) or Aurora C (Ki = 4.6 nM); inhibits proliferation of clear cell renal carcinoma (IC50 = 2/M phase

MK-0457 – 250 mg

Brand:
Cayman
CAS:
639089-54-6
Storage:
-20
UN-No:
Non-Hazardous - /

The Aurora kinases (A, B, and C) are a family of serine-threonine kinases that regulate various stages of mitotic function. With significant roles in cell cycle and cell division, Aurora kinase gene amplification and overexpression are linked to tumorigenesis.{18438} MK-0457 is a potent pan-Aurora kinase inhibitor but favors Aurora A (Ki = 0.6 nM) over Aurora B (Ki = 18 nM) or Aurora C (Ki = 4.6 nM).{17545} It shows selectivity against a panel of more than 190 different protein kinases.{17545} MK-0457 effectively inhibits proliferation of several different cell lines of clear cell renal carcinoma (IC50s = 2/M phase.{18438}  

 

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Description

A potent pan-Aurora kinase inhibitor that favors Aurora A (Ki = 0.6 nM) over Aurora B (Ki = 18 nM) or Aurora C (Ki = 4.6 nM); inhibits proliferation of clear cell renal carcinoma (IC50 = 2/M phase

Formal name: N-[4-[[4-(4-methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]-cyclopropanecarboxamide

Synonyms:  Tozasertib|VX-680

Molecular weight: 464.6

CAS: 639089-54-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Aurora||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Aurora Signaling

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