BMS-986115

DRACPC ID  DRACPC0052

Active Ingredients   BMS-986115

Description  An orally bioavailable, gamma secretase (GS) and pan-Notch inhibitor, with potential antineoplastic activity. Upon administration, GS/pan-Notch inhibitor AL102 binds to GS and blocks the proteolytic cleavage and release of the Notch intracellular domain (NICD), which would normally follow ligand binding to the extracellular domain of the Notch receptor. This prevents both the subsequent translocation of NICD to the nucleus to form a transcription factor complex and the expression of Notch-regulated genes. This results in the induction of apoptosis and the inhibition of growth of tumor cells that overexpress Notch. Overexpression of the Notch signaling pathway plays an important role in tumor cell proliferation and survival. The integral membrane protein GS is a multi-subunit protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors, at residues within their transmembrane domains and leads to their activation.

Synonyms  GS/pan-Notch Inhibitor AL102; AL 102; AL-102; BMS-986115

Type  Small Molecule

Disease  Various Advanced Cancer

Classification

  

GS/pan-Notch Inhibitor Amino acid and derivative

Structure Information


Molecular Formula  C26H25F7N4O3

Molecular Weight  574.5

Active Sequence  Not available

Sequence Length  Not available

Modification  Not available

Structure

 

Show IUPAC/InChI/SMILES

IUPAC Name  (2S,3R)-N'-[(3S)-5-(3-fluorophenyl)-9-methyl-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]-2,3-bis(3,3,3-trifluoropropyl)butanediamide

InChI  InChI=1S/C26H25F7N4O3/c1-13-4-2-7-18-19(13)36-24(40)22(35-20(18)14-5-3-6-15(27)12-14)37-23(39)17(9-11-26(31,32)33)16(21(34)38)8-10-25(28,29)30/h2-7,12,16-17,22H,8-11H2,1H3,(H2,34,38)(H,36,40)(H,37,39)/t16-,17+,22+/m0/s1

InChI_Key SRJNRAQUSAVENA-GSHUGGBRSA-N

SMILES  O=C(N)[C@@H](CCC(F)(F)F)[C@@H](CCC(F)(F)F)C(N[C@@H]1C(NC2=C(C)C=CC=C2C(C3=CC=CC(F)=C3)=N1)=O)=O

External Codes


PubChem CID  73388393

DrugBank Accession Number  DB13126

NCI Thesaurus Code  C118573  

UNII  LSK1L593UU   GSRS

CAS  1584647-27-7



Drug approval


Drug indication
    BMS-986115 has been used in trials studying the treatment of Various Advanced Cancer.

    The drug is not approved.

ClinicalTrials.gov Identifier Title Condition or disease Phase Purpose
NCT01986218 Phase I Ascending Multiple-Dose Study to Evaluate the Safety, Pharmacokinetics and Pharmacodynamics of BMS-986115 in Subjects With Advanced Solid Tumors Various Advanced Cancer Phase 1 Treatment

    More clinical information is obtained from ClinicalTrials.gov.





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