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PHA-848125

PHA-848125 structure

CAS No:
802539-81-7
Formula:
C25H32N8O
Chemical Name:
PHA-848125
Synonyms:
PHA-848125;4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;Milciclib;PHA-848125 (Milciclib);Milciclib (PHA-848125);N,1,4,4-tetramethyl-8-(4-(4-methylpiperazin-1-yl)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide PHA 848125;4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]
Categories:
Biochemical Engineering > Inhibitors

Description

Milciclib (PHA-848125) is a potent, dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.

Milciclib Maleate is under investigation in clinical trial NCT01301391 (Study of Oral PHA-848125AC in Patients With Malignant Thymoma Previously Treated With Multiple Lines of Chemotherapy).|Milciclib is an orally bioavailable inhibitor of cyclin-dependent kinases (CDKs) and tropomyosin receptor kinase A (TRKA), with potential antineoplastic activity. CDK2/TRKA inhibitor PHA-848125 AC potently inhibits cyclin-dependent kinase 2 (CDK2) and exhibits activity against other CDKs including CDK1 and CDK4, in addition to TRKA. Inhibition of these kinases may result in cell cycle arrest and apoptosis of tumor cells that express these kinases. CDKs are serine/threonine kinases involved in regulation of the cell cycle and may be overexpressed in some cancer cell types. The neurotrophin receptor TRKA is mutated in a variety of cancer cell types.

PHA-848125 Basic Attributes

Molecular Weight：

460.59

Exact Mass：

460.269897

EC Number：

-0

UNII：

688000M8S8

DSSTox ID：

DTXSID80230186

NCI Thesaurus Code：

C148410

Characteristics

PSA：

91.2

XLogP3：

2.8

Density：

1.3±0.1 g/cm3

Melting Point：

190 °C

Refractive Index：

1.692

Drug Information

MeSH Entry Terms：

miliciclib

Computed Properties

Molecular Weight:460.6
XLogP3:2.8
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:4
Exact Mass:460.26990767
Monoisotopic Mass:460.26990767
Topological Polar Surface Area:91.2
Heavy Atom Count:34
Complexity:718
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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CAS No.: 802539-81-7

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