General Information of Drug (ID: DMUNJZB)

Drug Name
UCN-01 Drug Info
Synonyms
UCN; UCN01; Ucn 01; KRX-0601; KW-2401; UCN-02; (5s,6r,7r,9r,16r)-16-hydroxy-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-5h,14h-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-one; 7-Hydroxystaurosporine; 7-hydroxystaurosporine (UCN-01)
Indication
Disease Entry ICD 11 Status REF
Non-small-cell lung cancer 2C25.Y Phase 2 [1]
Therapeutic Class
Anticancer Agents
Cross-matching ID
PubChem CID
72271
CAS Number
CAS 112953-11-4
TTD Drug ID
DMUNJZB
VARIDT Drug ID
DR01437

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Checkpoint kinase-1 (CHK1) TTTU902 CHK1_HUMAN Inhibitor [2] , [3] , [4] , [5] , [6]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Phase 2 [7]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Checkpoint kinase-1 (CHK1) DTT CHEK1 4.267 4.629 3.739 5.322
Breast cancer resistance protein (ABCG2) DTP BCRP 6.732 7.513 6.326 9.277
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Non-small-cell lung cancer
ICD Disease Classification 2C25.Y
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Checkpoint kinase-1 (CHK1) DTT CHEK1 7.22E-191 1.43 4.74
Breast cancer resistance protein (ABCG2) DTP BCRP 3.87E-47 -1.28E+00 -1.63E+00
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 ClinicalTrials.gov (NCT00082017) UCN-01 (7-Hydroxystaurosporine) to Treat Relapsed T-Cell Lymphomas. U.S. National Institutes of Health.
2 Characterization of an inhibitory dynamic pharmacophore for the ERCC1-XPA interaction using a combined molecular dynamics and virtual screening app... J Mol Graph Model. 2009 Sep;28(2):113-30.
3 CHK1 inhibition as a strategy for targeting Fanconi Anemia (FA) DNA repair pathway deficient tumors. Mol Cancer. 2009 Apr 16;8:24.
4 UCN-01 inhibits p53 up-regulation and abrogates gamma-radiation-induced G(2)-M checkpoint independently of p53 by targeting both of the checkpoint kinases, Chk2 and Chk1. Cancer Res. 2002 Oct 15;62(20):5743-8.
5 The PI3K/Akt pathway as a target in the treatment of hematologic malignancies. Anticancer Agents Med Chem. 2009 Jun;9(5):550-9.
6 Cyclin-dependent kinase inhibitors as potential targeted anticancer agents. Invest New Drugs. 2009 Dec;27(6):586-94.
7 Pharmacogenomic importance of ABCG2. Pharmacogenomics. 2008 Aug;9(8):1005-9.