Cyclapolin 9

Names

[ Name ]:
Cyclapolin 9

[Synonym ]:
5-methylpyridazinecarboxamide 4-oxide
5-methyl-pyrazin-2-carboxamide-4-oxide
2-carbamoyl-5-methylpyrazine 4-oxide
Pyrazinecarboxamide,5-methyl-,4-oxide
7-nitro-3-oxy-5-trifluoromethyl-benzothiazole-2-carboxylic acid amide
L-NMMA acetate
5-methyl-pyrazine-2-carboxamide-4-oxide
2-Carbamoyl-5-methylpyrazin-4-oxid
5-methyl-4-oxy-pyrazine-2-carboxylic acid amide
2-Carbamoyl-7-nitro-5-trifluormethyl-benzothiazole-N-oxide

Biological Activity

[Description]:

Cyclapolin 9 is a potent, selective and ATP-competitive polo-like kinase 1 (PLK1) inhibitor with an IC50 of 500 nM. Cyclapolin 9 is inactive against other kinases[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Polo-like Kinase (PLK)

[Target]

PLK1:500 nM (IC50)

[In Vitro]

Cyclapolin 9 (3 μM) reduces electric field stimulation (EFS)-induced contractions of prostate strips. The α1-adrenergic smooth muscle contraction in the human prostate can be inhibited by Cyclapolin 9[1].

[References]

[1]. Martin Hennenberg, et al. Inhibition of Prostate Smooth Muscle Contraction by Inhibitors of Polo-Like Kinases. Front Physiol. 2018 Jun 15;9:734.

[2]. Campbell McInnes, et al. Inhibitors of Polo-like kinase reveal roles in spindle-pole maintenance. Nat Chem Biol. 2006 Nov;2(11):608-17.

Chemical & Physical Properties

[ Molecular Formula ]:
C₉H₄F₃N₃O₄S

[ Molecular Weight ]:
307.20600

[ Exact Mass ]:
306.98700

[ PSA ]:
142.61000

[ LogP ]:
3.57920

Safety Information

[ HS Code ]:
2934999090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%