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

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.

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BETd-260

BETd-260 Chemische Struktur

CAS. Nr. : 2093388-62-4

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Based on 4 publication(s) in Google Scholar

BETd-260 Related Antibodies

Top Publications Citing Use of Products

Alle PROTACs Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biologische Aktivität

  • Protokoll

  • Reinheit & Dokumentation

  • Verweise

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Beschreibung

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)

Cellular Effect
Cell Line Type Value Description References
RS4-11 IC50
0.051 1
Compound: 23
Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28339196]
MOLM-13 IC50
2.2 1
Compound: 23
Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28339196]
MOLM-13 IC50
2.2 1
Compound: 23
Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28339196]
RS4-11 IC50
0.051 1
Compound: 23
Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28339196]
MOLM-13 IC50
2.2 1
Compound: 23
Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28339196]
RS4-11 IC50
0.051 1
Compound: 23
Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 28339196]
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].

MedChemExpress (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].

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

798.89

Formel

C43H46N10O6
CAS. Nr.
Appearance

Solid

Color

Off-white to yellow

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
Versand

Shipping with dry ice.
Speicherung

-80°C, protect from light, stored under nitrogen
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 25 mg/mL (31.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

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

    This protocol yields a clear solution of ≥ 0.83 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 (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation

Purity: 99.68%

SDS (393 KB)

COA (248 KB) HNMR (139 KB) RP-HPLC (227 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
Verweise
Zellassay
[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 hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Tierverwaltung
[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 hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Verweise

Complete Stock Solution Preparation Table

* 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2517 mL 6.2587 mL 12.5174 mL 31.2934 mL
5 mM 0.2503 mL 1.2517 mL 2.5035 mL 6.2587 mL
10 mM 0.1252 mL 0.6259 mL 1.2517 mL 3.1293 mL
15 mM 0.0834 mL 0.4172 mL 0.8345 mL 2.0862 mL
20 mM 0.0626 mL 0.3129 mL 0.6259 mL 1.5647 mL
25 mM 0.0501 mL 0.2503 mL 0.5007 mL 1.2517 mL
30 mM 0.0417 mL 0.2086 mL 0.4172 mL 1.0431 mL
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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.

Keywords:

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

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