1. PROTAC
    Epigenetics
  2. PROTAC
    Epigenetic Reader Domain
  3. BETd-246

BETd-246 

Cat. No.: HY-115568 Purity: 98.03%
Handling Instructions

BETd-246 is a second-generation BET bromodomain (BRD) inhibitor, exhibiting superior selectivity, potency and antitumor activity.

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

BETd-246 Chemical Structure

BETd-246 Chemical Structure

CAS No. : 2140289-17-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 989 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 950 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BETd-246 is a second-generation BET bromodomain (BRD) inhibitor, exhibiting superior selectivity, potency and antitumor activity[1].

IC50 & Target

BET BRD[1].

In Vitro

BETd-246 treatment (0-100 nM, 1-3 h) causes a dose-dependent depletion of BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation.
BETd-246 (100 nM, 24/48 hours) displays strong growth inhibition and apoptosis induction activity in MDA-MB-468 cell lines. BETd-246 induces a rapid and time-dependent downregulation of MCL1 protein in all the TNBC cell lines evaluated. BETd-246 induces much stronger apoptosis than BETi-211.
BETd-246 (100 nM, 24 hours) induces pronounced cell cycle arrest and apoptosis in TNBC cell lines[1].

Cell Proliferation Assay[1]

Cell Line: MDA-MB-468 cells
Concentration: 100 nM
Incubation Time: 24 or 48 hours
Result: Displayed strong growth inhibition and apoptosis induction activity in TNBC cell lines.

Cell Cycle Analysis[1]

Cell Line: Human TNBC cells
Concentration: 100 nM
Incubation Time: 24 hours
Result: Induced pronounced cell cycle arrest and apoptosis in TNBC cell lines.

Western Blot Analysis[1]

Cell Line: Human TNBC cells
Concentration: 0-100 nM
Incubation Time: 1-3 hours
Result: Caused a dose-dependent depletion of BRD2, BRD3 and BRD4.
In Vivo

BETd-246 (5 mg/kg, IV, 3 times per week for 3 weeks) treatment effectively inhibits WHIM24 tumor growth, similar to the antitumor activity of BETi-211 with higher dosage and more frequently administration. The treatment of 10 mg/kg induces partial tumor regression during treatment without apparent toxicity. BETd-246 has very limited drug exposure in the xenograft tumor tissue in MDA-M-231and MDA-MB-468 models[1].

Animal Model: “Washington Human in Mouse (WHIM)” (PDX) model developed from a patient with treatment-resistant breast cancer (ESRE380Q, PR- and HER2-))[1].
Dosage: 5, 10 mg/kg
Administration: IV, 3 times per week for 3 weeks.
Result: Effectively inhibited WHIM24 tumor growth.
Molecular Weight

946.02

Formula

C₄₈H₅₅N₁₁O₁₀

CAS No.

2140289-17-2

SMILES

O=C(C1=NC(NC2=CC(C3CC3)=NN2CC)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1)NCCCOCCOCCOCCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (211.41 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0571 mL 5.2853 mL 10.5706 mL
5 mM 0.2114 mL 1.0571 mL 2.1141 mL
10 mM 0.1057 mL 0.5285 mL 1.0571 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 5 mg/mL (5.29 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • 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-246
Cat. No.:
HY-115568
Quantity: