Art. -Nr.: HY-115568

BETd-246

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity.
(Pink: BET ligand (HY-122703); Blue: Cereblon ligand (HY-103596); Black: linker (HY-128844)).

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Reinheit: 98.34%
CAS. Nr.: 2140289-17-2
Formel: C₄₈H₅₅N₁₁O₁₀
Molecular Weight:946.02

Speicherung:

-20°C, stored under nitrogen

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

BETd-246 Chemical Structure

CAS. Nr.: 2140289-17-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity^[1]. (Pink: BET ligand (HY-122703); Blue: Cereblon ligand (HY-103596); Black: linker (HY-128844)).

IC₅₀ & Target

BET BRD^[1].

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Burkitts lymphoma cell	GI₅₀	0.4 μM Compound: BETd-246; 6	Antiproliferative activity against human Burkitts lymphoma cells Antiproliferative activity against human Burkitts lymphoma cells	[PMID: 36202064]
MDA-MB-468	IC₅₀	<10 nM Compound: BETd-246; 6	Antiproliferative activity against human MDA-MB-468 cells Antiproliferative activity against human MDA-MB-468 cells	[PMID: 36202064]
MV4-11	IC₅₀	1.24 μM Compound: BETd-246; 6	Cytotoxicity against human MV4-11 cells Cytotoxicity against human MV4-11 cells	[PMID: 36202064]
MV4-11	IC₅₀	6 nM Compound: BETd-246; 6	Cytotoxicity against human MV4-11 cells measured after 96 hrs Cytotoxicity against human MV4-11 cells measured after 96 hrs	[PMID: 36202064]
NAMALVA	GI₅₀	0.34 μM Compound: BETd-246; 6	Antiproliferative activity against human NAMALVA cells Antiproliferative activity against human NAMALVA cells	[PMID: 36202064]

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].

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

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].

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

Animal Model:

“Washington Human in Mouse (WHIM)” (PDX) model developed from a patient with treatment-resistant breast cancer (ESR^E380Q, PR- and HER2-))^[1].
Dosage:

5, 10 mg/kg
Administration:

IV, 3 times per week for 3 weeks.
Result:

Effectively inhibited WHIM24 tumor growth.

Chemical Information

CAS. Nr. 2140289-17-2
Appearance Solid
Molecular Weight 946.02
Formel C₄₈H₅₅N₁₁O₁₀
Color Light yellow to yellow
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

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

Publications (2)

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Structure

PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]

2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
Biochem Biophys Res Commun

Accelerating PROTAC drug discovery: Establishing a relationship between ubiquitination and target protein degradation. [Abstract]

2022 Nov 5:628:68-75. PMID: 36084553

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 200 mg/mL (211.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Bai L, et al. Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer. Cancer Res. 2017 May 1;77(9):2476-2487. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0571 mL	5.2853 mL	10.5706 mL	26.4265 mL
	5 mM	0.2114 mL	1.0571 mL	2.1141 mL	5.2853 mL
	10 mM	0.1057 mL	0.5285 mL	1.0571 mL	2.6427 mL
	15 mM	0.0705 mL	0.3524 mL	0.7047 mL	1.7618 mL
	20 mM	0.0529 mL	0.2643 mL	0.5285 mL	1.3213 mL
	25 mM	0.0423 mL	0.2114 mL	0.4228 mL	1.0571 mL
	30 mM	0.0352 mL	0.1762 mL	0.3524 mL	0.8809 mL
	40 mM	0.0264 mL	0.1321 mL	0.2643 mL	0.6607 mL
	50 mM	0.0211 mL	0.1057 mL	0.2114 mL	0.5285 mL
	60 mM	0.0176 mL	0.0881 mL	0.1762 mL	0.4404 mL
	80 mM	0.0132 mL	0.0661 mL	0.1321 mL	0.3303 mL
	100 mM	0.0106 mL	0.0529 mL	0.1057 mL	0.2643 mL

Keywords

BETd-246

2 Cited Publications

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BETd-246

PROTAC Library

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) BETd-246

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BETd-246

PROTAC Library

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) BETd-246

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BETd-246 Related Classifications

Art. -Nr.: HY-115568