ZBC260
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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.


Chemical Structure

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ZBC260
CAS# 2093388-62-4

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

Price and Availability

Size Price Availability Quantity
25.0mg USD 750.0 1 month
50.0mg USD 1350.0 1 month
100.0mg USD 1950.0 1 month
200.0mg USD 2950.0 1 month
500.0mg USD 4650.0 1 month
1.0g USD 5950.0 1 month
2.0g USD 9950.0 1 month
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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

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).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 798.905 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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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.

ZBC260

25.0mg / USD 750.0


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