| Drug General Information |
| Drug ID |
D07DTV
|
| Former ID |
DCL000058
|
| Drug Name |
AT7519
|
| Synonyms |
LZE; AT 7519, AT7519; AT-7519; 4-[(2,6-dichlorobenzoyl)amino]-N-(4-piperidyl)-2H-pyrazole-3-carboxamide
|
| Drug Type |
Small molecular drug
|
| Indication |
Solid tumours [ICD9: 140-199, 210-229; ICD10:C00-D48]
|
Discontinued in Phase 2 |
[1],
[2],
[3]
|
|---|
| Therapeutic Class |
Anticancer Agents
|
| Company |
Astex Therape.
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C16H17Cl2N5O2
|
| InChI |
InChI=1S/C16H17Cl2N5O2/c17-10-2-1-3-11(18)13(10)15(24)22-12-8-20-23-14(12)16(25)21-9-4-6-19-7-5-9/h1-3,8-9,19H,4-7H2,(H,20,23)(H,21,25)(H,22,24)
|
| InChIKey |
OVPNQJVDAFNBDN-UHFFFAOYSA-N
|
| CAS Number |
CAS 902135-91-5
|
| PubChem Compound ID |
|
| PubChem Substance ID |
16428822, 44379310, 50096508, 56269605, 74576064, 99437204, 99444613, 103643679, 124757315, 125164119, 135333280, 135685970, 135685971, 135685992, 135685993, 135727820, 136340234, 136367456, 136368084, 137041629, 137275934, 137275935, 141610040, 143499366, 144115640, 152234931, 152258863, 152344091, 160647712, 160969196, 162011646, 162202560, 162205110, 163642676, 163907975, 172918159, 174530768, 177748954, 178102290, 180371628, 185990438, 198975169, 223405959, 223704734, 224043268, 227215649, 242060190, 245357213, 245380549, 251910783
|
| Target and Pathway |
| Target(s) |
Cell division protein kinase 2 |
Target Info |
Inhibitor |
[4]
|
|---|
|
KEGG Pathway
|
FoxO signaling pathway
|
|
Cell cycle
|
|
Oocyte meiosis
|
|
p53 signaling pathway
|
|
PI3K-Akt signaling pathway
|
|
Progesterone-mediated oocyte maturation
|
|
Hepatitis B
|
|
Measles
|
|
Herpes simplex infection
|
|
Epstein-Barr virus infection
|
|
Pathways in cancer
|
|
Viral carcinogenesis
|
|
Prostate cancer
|
|
Small cell lung cancer
|
|
NetPath Pathway
|
TCR Signaling Pathway
|
|
PANTHER Pathway
|
p53 pathway
|
|
p53 pathway feedback loops 2
|
|
Pathway Interaction Database
|
Regulation of nuclear SMAD2/3 signaling
|
|
Signaling events mediated by PRL
|
|
p73 transcription factor network
|
|
E2F transcription factor network
|
|
ATR signaling pathway
|
|
mTOR signaling pathway
|
|
IL2-mediated signaling events
|
|
FoxO family signaling
|
|
FOXM1 transcription factor network
|
|
BARD1 signaling events
|
|
p53 pathway
|
|
Regulation of retinoblastoma protein
|
|
Reactome
|
G0 and Early G1
|
|
Activation of ATR in response to replication stress
|
|
Regulation of APC/C activators between G1/S and early anaphase
|
|
SCF(Skp2)-mediated degradation of p27/p21
|
|
Senescence-Associated Secretory Phenotype (SASP)
|
|
DNA Damage/Telomere Stress Induced Senescence
|
|
Processing of DNA double-strand break ends
|
|
G2 Phase
|
|
Orc1 removal from chromatin
|
|
Cyclin E associated events during G1/S transition
|
|
Cyclin A/B1 associated events during G2/M transition
|
|
p53-Dependent G1 DNA Damage Response
|
|
Cyclin A:Cdk2-associated events at S phase entry
|
|
Meiotic recombination
|
|
Factors involved in megakaryocyte development and platelet production
|
|
WikiPathways
|
DNA Damage Response
|
|
ID signaling pathway
|
|
DNA Replication
|
|
G1 to S cell cycle control
|
|
M/G1 Transition
|
|
S Phase
|
|
Meiotic Recombination
|
|
Aryl Hydrocarbon Receptor
|
|
ATM Signaling Pathway
|
|
Retinoblastoma (RB) in Cancer
|
|
Spinal Cord Injury
|
|
Integrated Pancreatic Cancer Pathway
|
|
Oncostatin M Signaling Pathway
|
|
Prostate Cancer
|
|
Signaling Pathways in Glioblastoma
|
|
TSH signaling pathway
|
|
Integrated Breast Cancer Pathway
|
|
Integrated Cancer pathway
|
|
Synthesis of DNA
|
|
Regulation of DNA replication
|
|
Mitotic G2-G2/M phases
|
|
Mitotic G1-G1/S phases
|
|
Factors involved in megakaryocyte development and platelet production
|
|
Cell Cycle
|
|
APC/C-mediated degradation of cell cycle proteins
|
|
Cell Cycle Checkpoints
|
|
miRNA Regulation of DNA Damage Response
|
| References |
| REF 1 | AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition. Oncogene. 2010 Apr 22;29(16):2325-36. |
|---|
| REF 2 | Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem. 2010 Mar 1;18(5):1844-53. |
|---|
| REF 3 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5662). |
|---|
| REF 4 | Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Mol Cancer Ther. 2009 Feb;8(2):324-32. Epub 2009 Jan 27. |
|---|
