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Home > Encyclopedia > 4-[(2,6-dichlorobenzoyl)amino]-N-4-piperidinyl1H-pyrazole-3-carboxamide

4-[(2,6-dichlorobenzoyl)amino]-N-4-piperidinyl1H-pyrazole-3-carboxamide

4-[(2,6-dichlorobenzoyl)amino]-N-4-piperidinyl1H-pyrazole-3-carboxamide structure

4-[(2,6-dichlorobenzoyl)amino]-N-4-piperidinyl1H-pyrazole-3-carboxamide 

structure
  • CAS No:

    844442-38-2

  • Formula:

    C16H17Cl2N5O2

  • Chemical Name:

    4-[(2,6-dichlorobenzoyl)amino]-N-4-piperidinyl1H-pyrazole-3-carboxamide

  • Synonyms:

    4-[(2,6-dichlorobenzoyl)amino]-N-4-piperidinyl1H-pyrazole-3-carboxamide;4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide;AT 7519 N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide;N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide AT 7519;AT7519, >=99%;N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide;CS-1664;1H-Pyrazole-3-carboxamide, 4-[(2,6-dichlorobenzoyl)amino]-N-4-piperidinyl-

  • Categories:

    Biochemical Engineering  >  Inhibitors

Description

AT7519 as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.


4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-pyrazole-3-carboxamide is a member of the class of pryrazoles that is 4-amino-1H-pyrazole-3-carboxylic acid in which the primary amino group has been acylated by a 2,6-dichlorobenzoyl group and in which the carboxylic acid has been converted into a carboxamide by formal condensation with the primary amino group of 4-aminopiperidine. It has a role as an EC 2.7.11.22 (cyclin-dependent kinase) inhibitor and an antineoplastic agent. It is a secondary carboxamide, a member of pyrazoles, a dichlorobenzene and a member of piperidines.|AT7519 is a selective inhibitor of certain Cyclin Dependent Kinases (CDKs) leading to tumour regression. It is developed by Astex for the treatment of solid tumours and haematological malignancies.|CDK Inhibitor AT7519 is an orally bioavailable small molecule with potential antineoplastic activity. AT7519M selectively binds to and inhibits cyclin dependent kinases (CDKs), which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation. CDKs are serine/threonine kinases involved in regulation of the cell cycle and may be overexpressed in some types of cancer cells.

4-[(2,6-dichlorobenzoyl)amino]-N-4-piperidinyl1H-pyrazole-3-carboxamide Basic Attributes

382.24

382.24

X1BF92PW9T

DTXSID30233420

C64761

White to off-white

Characteristics

98.9

2.6

1.48±0.1 g/cm3(Predicted)

586.0±50.0 °C(Predicted)

308.2±30.1 °C

1.654

11.10±0.70(Predicted)

Store at -20°C

Drug Information

Investigated for use/treatment in leukemia (unspecified), lymphoma (unspecified), myelodysplastic syndrome, and solid tumors.

AT7519 is a selective inhibitor of certain Cyclin Dependent Kinases (CDKs) leading to tumour regression.

4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide

4-[(2,6-dichlorobenzoyl)amino]-N-4-piperidinyl1H-pyrazole-3-carboxamide Use and Manufacturing

AT-7519 is a small-molecule inhibitor of cyclin-dependent kinases (CDK). AT-7519 caused cell cycle arrest followed by apoptosis in human tumor cells and inhibited tumor growth in human tumor xenograft models. AT-7519 is being studied for its potential therapeutic benefits in cancer patients.

Computed Properties

Molecular Weight:382.2
XLogP3:2.6
Hydrogen Bond Donor Count:4
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:4
Exact Mass:381.0759302
Monoisotopic Mass:381.0759302
Topological Polar Surface Area:98.9
Heavy Atom Count:25
Complexity:479
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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