1. Epigenetics
    PROTAC
  2. Epigenetic Reader Domain
    PROTAC
  3. BETd-260

BETd-260 (Synonyms: ZBC 260)

Cat. No.: HY-101519 Purity: 99.35%
Handling Instructions

BETd-260 is a potent BET degrader based on PROTAC technology, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line.

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

BETd-260 Chemical Structure

BETd-260 Chemical Structure

CAS No. : 2093388-62-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 659 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2400 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BETd-260 is a potent BET degrader based on PROTAC technology, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line.

IC50 & Target

BRD4[1]
PROTAC

In Vitro

BETd-260 (ZBC260; Compound 23) 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].

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].

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

H2O : < 0.1 mg/mL (insoluble)

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

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
Molecular Weight

798.89

Formula

C₄₃H₄₆N₁₀O₆

CAS No.

2093388-62-4

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

Room temperature in continental US; may vary elsewhere

Purity: 99.35%

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
BETd-260
Cat. No.:
HY-101519
Quantity:

BETd-260

Cat. No.: HY-101519