OTX-015

• CAT Number: I002559
• CAS Number: 202590-98-5
• Molecular Formula: C25H22ClN5O2S
• Molecular Weight: 492
• Purity: ≥95%
• Synonyms: birabresib
• Target: Epigenetic Reader Domain
• Solubility: DMSO: ≥ 49 mg/mL
• Storage: Store at -20°C
• IC50: 0.192 uM (DLBCL cell lines)
• IUPAC Name: 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]-N-(4-hydroxyphenyl)acetamide
• InChI: InChI=1S/C25H22ClN5O2S/c1-13-14(2)34-25-22(13)23(16-4-6-17(26)7-5-16)28-20(24-30-29-15(3)31(24)25)12-21(33)27-18-8-10-19(32)11-9-18/h4-11,20,32H,12H2,1-3H3,(H,27,33)/t20-/m0/s1
• InChIKey: GNMUEVRJHCWKTO-FQEVSTJZSA-N
• SMILES: CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NC4=CC=C(C=C4)O)C5=CC=C(C=C5)Cl)C

OTX-015(CAT: I002559), also known as birabresib, is a small molecule inhibitor of bromodomain and extra-terminal (BET) proteins. It selectively targets the bromodomain proteins BRD2, BRD3, and BRD4, which are involved in the regulation of gene expression. By inhibiting BET proteins, OTX-015 interferes with the binding of BET proteins to acetylated histones, disrupting the formation of transcriptional complexes and leading to the downregulation of specific genes, including those involved in oncogenesis. OTX-015 has shown potential as an anticancer agent, particularly in hematologic malignancies. Clinical trials have evaluated its efficacy and safety in various types of cancer, including leukemia and lymphoma.

Overview of Clinical Research

OTX-015 is under investigation in clinical trial NCT02698176 (A Dose Exploration Study With MK-8628 in Participants With Selected Advanced Solid Tumors (MK-8628-006)). The Phase I clinical trial:Dose-finding Study of the Bromodomain (Brd) Inhibitor OTX-015 in Hematological Malignancies is on going.

Reference

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