BETd-260

CAS No. 2093388-62-4

BETd-260( ZBC 260 | ZBC260 | BETd 260 )

Catalog No. M13282 CAS No. 2093388-62-4

BETd-260 (ZBC260, BETd260) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    BETd-260
  • Note
    Research use only, not for human use.
  • Brief Description
    BETd-260 (ZBC260, BETd260) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.
  • Description
    BETd-260 (ZBC260, BETd260) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL; effectively degrades BRD4 protein at 30 pM in the RS4;11 leukemia cell line, achieves an IC50 of 51 pM in inhibition of RS4;11 cell growth and induces rapid tumor regression in vivo against RS4;11 xenograft tumors.
  • In Vitro
    BETd-260 (ZBC260; Compound 23) is capable of inducing degradation of BRD2, BRD3, and BRD4 proteins at 30–100 pM in the RS4;11 leukemia cells. BETd-260 shows inhibitory activity against the growth of RS4;11 leukemia cells and MOLM-13 cells with IC50s of 51 pM and 2.2 nM, respectively, and induces apoptosis in both RS4;11 and MOLM-13 cell lines at 3-10 nM.BETd-260 reciprocally modulates the expression of several apoptotic genes in HCC cells, i.e., suppressing the expression of anti-apoptotic Mcl-1, Bcl-2, c-Myc, and XIAP, whereas increasing the expression of pro-apoptotic Bad.
  • In Vivo
    BETd-260 (5 mg/kg, i.v., every other day, thrice a week for 3 weeks) causes rapid tumor regression with a maximum of >90% regression in mice bearing RS4;11 xenograft tumors, and with no body weight loss or other signs of toxicity in mice. BETd-260 (5 mg/kg, i.v.) degrades the BRD2, BRD3, and BRD4 proteins for more than 24 h, with robust cleavage of PARP and caspase-3, and strong down-regulation of c-Myc protein in RS4;11 xenograft mice model.
  • Synonyms
    ZBC 260 | ZBC260 | BETd 260
  • Pathway
    PROTACs
  • Target
    PROTAC
  • Recptor
    PROTAC
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    2093388-62-4
  • Formula Weight
    798.905
  • Molecular Formula
    C43H46N10O6
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 25 mg/mL 31.29 mM;H2O : < 0.1 mg/mL
  • SMILES
    O=C(N1)CCC(N(CC2=C3C=CC=C2CCCCCNC(C4=NC5=C(C(NC6=CC(C7CC7)=NN6CC)=N4)C8=CC(OC)=C(C9=C(C)ON=C9C)C=C8N5)=O)C3=O)C1=O
  • Chemical Name
    4-((3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino)-7-(3,5-dimethylisoxazol-4-yl)-N-(5-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)pentyl)-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Zhou B, et al. J Med Chem. 2017 Mar 24. doi: 10.1021/acs.jmedchem.6b01816.
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