General Information of Drug (ID: DMEGOQP)

Drug Name
RGB-286638 Drug Info
Synonyms
GPC-286199; RGB-286199; RGB-344064; Non-selective CDK inhibitors, Agennix; Non-selective CDK inhibitors, GPC Biotech; Non-selective cyclin dependent kinase inhibitors, Agennix; Non-selective cyclin dependent kinase inhibitors, GPC Biotech
Indication
Disease Entry ICD 11 Status REF
Haematological malignancy 2B33.Y Phase 1 [1]
Cross-matching ID
PubChem CID
11285001
CAS Number
CAS 784210-87-3
TTD Drug ID
DMEGOQP

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Cyclin-dependent kinase 1 (CDK1) TTH6V3D CDK1_HUMAN Inhibitor [2]
Cyclin-dependent kinase 2 (CDK2) TT7HF4W CDK2_HUMAN Inhibitor [2]
Cyclin-dependent kinase 3 (CDK3) TTMYWL7 CDK3_HUMAN Inhibitor [2]
Cyclin-dependent kinase 4 (CDK4) TT0PG8F CDK4_HUMAN Inhibitor [3]
Cyclin-dependent kinase 9 (CDK9) TT1LVF2 CDK9_HUMAN Inhibitor [2]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Cyclin-dependent kinase 1 (CDK1) DTT CDK1 2.036 5.914 4.781 5.914
Cyclin-dependent kinase 9 (CDK9) DTT CDK9 5.597 5.711 5.221 5.776
Cyclin-dependent kinase 4 (CDK4) DTT CDK4 7.414 7.821 7.812 7.719
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 Haematological malignancy
ICD Disease Classification 2B33.Y
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Cyclin-dependent kinase 1 (CDK1) DTT CDK1 5.27E-108 1.97 3.12
Cyclin-dependent kinase 2 (CDK2) DTT CDK2 2.28E-06 0.12 0.19
Cyclin-dependent kinase 9 (CDK9) DTT CDK9 4.38E-01 -0.04 -0.1
Cyclin-dependent kinase 4 (CDK4) DTT CDK4 3.30E-72 0.65 2.39
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 URL: 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: 7744).
2 Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia. 2013 Dec;27(12):2366-75.
3 Liposarcoma: molecular genetics and therapeutics. Sarcoma. 2011;2011:483154.