2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain Apoptosis
  4. BETd-260

BETd-260  (Synonyms: ZBC 260)

Cat. No.: HY-101519 Purity: 99.59%
COA Handling Instructions

BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.

For research use only. We do not sell to patients.

BETd-260 Chemical Structure

BETd-260 Chemical Structure

CAS No. : 2093388-62-4

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10 mg USD 980 In-stock
25 mg USD 2100 In-stock
50 mg USD 3650 In-stock
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Based on 1 publication(s) in Google Scholar

BETd-260 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line[1]. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells[2].

IC50 & Target[1]

BRD4

<30 pM (IC50)

BRD2

30-100 pM (IC50)

BRD3

30-100 pM (IC50)

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[1].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

BETd-260 Related Antibodies
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

798.89

Appearance

Solid

Formula

C43H46N10O6
CAS No.
SMILES

CCN1N=C(C2CC2)C=C1NC3=NC(C(NCCCCCC4=CC=CC5=C4CN(C6C(NC(CC6)=O)=O)C5=O)=O)=NC7=C3C8=CC(OC)=C(C9=C(C)ON=C9C)C=C8N7
Shipping

Shipping with dry ice.
Storage

-80°C, protect from light, stored under nitrogen
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (31.29 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2517 mL 6.2587 mL 12.5174 mL
5 mM 0.2503 mL 1.2517 mL 2.5035 mL
10 mM 0.1252 mL 0.6259 mL 1.2517 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.83 mg/mL (1.04 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.83 mg/mL (1.04 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.59%

COA (250 KB) HNMR (515 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

In cell growth experiments, cells are seeded in 96-well cell culture plates at a density of 10000−20000 cells/well in 100 μL of culture medium. BETd-260 is serially diluted in the appropriate medium, and 100 μL of the diluted solution containing BETd-260 is added to the appropriate wells of the cell plate. After addition of BETd-260, the cells are incubated for 4 days at 37°C in an atmosphere of 5% CO2. Cell growth is evaluated by a lactate dehydrogenase-based WST-8 assay using a multimode microplate reader. The WST-8 reagent is added to the plate, incubated for at least 1 h, and read at 450 nm. The readings are normalized to the DMSO-treated cells, and the IC50 is calculated by nonlinear regression analysis using GraphPad Prism 6 software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
To develop xenograft tumors, 5 × 106 RS4;11 cells with 50% Matrigel are injected subcutaneously on the dorsal side of severe combined immunodeficient (SCID) mice, one tumor per mouse. When tumors reach appr 100 mm3, mice are randomly assigned to BETd-260 treatment and vehicle control groups. Animals are monitored daily for any signs of toxicity and weighed 2-3 times per week during the treatment and weighed at least weekly after BETd-260 treatment end. Tumor size is measured 2-3 times per week by electronic calipers during the treatment period and at least weekly after the treatment is end. Tumor volume is calculated as V = LW2/2, where L is the length and W is the width of the tumor[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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BETd-260 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

BETd-2602093388-62-4ZBC 260BETd260BETd 260ZBC260ZBC-260PROTACsEpigenetic Reader DomainApoptosisreaderRS4;11leukemiacellstumorregressionapoptoticInhibitorinhibitorinhibit

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