ZBC260

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407812

CAS#: 2093388-62-4

Description: ZBC260, also known as BETd-260, is a potent and selective BET inhibitor or BET degrader. ZBC260 effectively degrades BRD4 protein at concentrations as low as 30 pM in the RS4;11 leukemia cell line, achieves an IC50 value of 51 pM in inhibition of RS4;11 cell growth and induces rapid tumor regression in vivo against RS4;11 xenograft tumors. ZBC260 is a highly potent and efficacious BET degrader.


Price and Availability

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ZBC260 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 407812
Name: ZBC260
CAS#: 2093388-62-4
Chemical Formula: C43H46N10O6
Exact Mass: 798.3602
Molecular Weight: 798.905
Elemental Analysis: C, 64.65; H, 5.80; N, 17.53; O, 12.02


Synonym: ZBC260; ZBC 260; ZBC-260; BETd-260; BETd 260; BETd260.

IUPAC/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

InChi Key: UZXANFBIRSYHGO-UHFFFAOYSA-N

InChi Code: InChI=1S/C43H46N10O6/c1-5-53-34(20-30(50-53)25-13-14-25)46-39-37-27-19-33(58-4)28(36-22(2)51-59-23(36)3)18-31(27)45-38(37)48-40(49-39)42(56)44-17-8-6-7-10-24-11-9-12-26-29(24)21-52(43(26)57)32-15-16-35(54)47-41(32)55/h9,11-12,18-20,25,32H,5-8,10,13-17,21H2,1-4H3,(H,44,56)(H,47,54,55)(H2,45,46,48,49)

SMILES Code: 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


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic "readers" and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets for cancer and other human diseases. Recently, heterobifunctional small-molecule BET degraders have been designed based upon the proteolysis targeting chimera (PROTAC) concept to induce BET protein degradation


References

1: Zhou B, Hu J, Xu F, Chen Z, Bai L, Fernandez-Salas E, Lin M, Liu L, Yang CY,
Zhao Y, McEachern D, Przybranowski S, Wen B, Sun D, Wang S. Discovery of a
Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with
Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med
Chem. 2017 Mar 24. doi: 10.1021/acs.jmedchem.6b01816. [Epub ahead of print]
PubMed PMID: 28339196.