Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DM0YCPL)

• Drug Name: Bemcentinib Drug Info
• Synonyms: R428; 1037624-75-1; BGB324; R-428; BGB-324; UNII-0ICW2LX8AS; (S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine; CHEMBL3809489; SYN1131; CS-1046; HY-15150; QC-11751; R 428; W-5845; Bemcentinib [USAN]; R428 (BGB324); Bemcentinib (USAN/INN); BemcentinibR428BGB324); SCHEMBL1639904; GTPL10478; BGB 324; DTXSID70673109; 1-(6,7-dihydro-5H-benzo[2,3]cyclohepta[2,4-d]pyridazin-3-yl)-3-N-[(7S)-7-pyrrolidin-1-yl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-3-yl]-1,2,4-triazole-3,5-diamine; AMY16774; BCP21180; C30H34N8; EX-A1720; SYN-1131; BDBM50172079; NSC824183; s2841; WHO 10631; ZINC51951669; AKOS032947237; ACN-037541; DB12411; NSC-824183; SB16614; NCGC00386665-07; 1-(6,7-Dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N~3~-[(7S)-7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl]-1H-1,2,4-triazole-3,5-diamine; 1H-1,2,4-Triazole-3,5-diamine, 1-(6,7-dihydro-5H-benzo(6,7)cyclohepta(1,2-C)pyridazin-3-yl)-N3-((7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5H-benzocyclohepten-2-yl)-; AC-28444; AS-16270; KB-80319; D11438; Q27236818; BGB324; BGB-324; BGB 324; R 428; R-428; Bemcentinib; 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(S)-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulene-2-yl)-1H-1,2,4-triazole-3,5-diamine

Indication

Disease Entry	ICD 11	Status	REF
Myelodysplastic syndrome	2A37	Phase 2	[1]
Non-small-cell lung cancer	2C25.Y	Phase 2	[2]
Triple negative breast cancer	2C60-2C65	Phase 2	[3]

• Cross-matching ID:
  PubChem CID: 46215462
  CAS Number: CAS 1037624-75-1
  TTD Drug ID: DM0YCPL

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Tyrosine-protein kinase UFO (AXL)	TTZPY6J	UFO_HUMAN	Inhibitor	[4]

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

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Tyrosine-protein kinase UFO (AXL)	DTT	AXL	6.677	7.261	6.33	7.021

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

• The Studied Disease: Myelodysplastic syndrome
• ICD Disease Classification: 2A37

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Tyrosine-protein kinase UFO (AXL)	DTT	AXL	1.13E-65	-0.53	-2.04

References

• [1] ClinicalTrials.gov (NCT03824080) Evaluating the Efficacy and Safety of Bemcentinib in Patients With Myelodysplastic Syndromes. U.S. National Institutes of Health.
• [2] ClinicalTrials.gov (NCT03184571) Bemcentinib (BGB324) in Combination With Pembrolizumab in Patients With Advanced NSCLC. U.S. National Institutes of Health.
• [3] ClinicalTrials.gov (NCT03184558) Bemcentinib (BGB324) in Combination With Pembrolizumab in Patients With TNBC. U.S. National Institutes of Health.
• [4] AXL Targeting Abrogates Autophagic Flux and Induces Immunogenic Cell Death in Drug-Resistant Cancer Cells. J Thorac Oncol. 2020 Jun;15(6):973-999.