2. Epigenetics
  3. Epigenetic Reader Domain
  4. BET-IN-14

BET-IN-14 is an orally active pan BET inhibitor (IC50: 5.35 nM). BET-IN-14 has anti-cancer activity.

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

BET-IN-14 Chemical Structure

BET-IN-14 Chemical Structure

CAS No. : 2243669-93-2

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5 mg USD 890 In-stock
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Based on 1 publication(s) in Google Scholar

BET-IN-14 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

BET-IN-14 is an orally active pan BET inhibitor (IC50: 5.35 nM). BET-IN-14 has anti-cancer activity[1].

IC50 & Target

BET (IC50: 5.35 nM)
In Vitro

BET-IN-14 (Compound 171) (72 h) shows anti-tumor activity against various cancer cell lines (average IC50: 174.7 nM), especially in MM.1S, Ty-82, MV-4-11, and KG-1 cells[1].

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

BET-IN-14 Related Antibodies

Cell Viability Assay[1]

Cell Line: NCI-H522, RKO, NCI-H1299, MM.1S, Ty-82, MV-4-11, and KG-1 cells
Concentration: 0-1 μM approximately
Incubation Time: 72 h
Result: Showed anti-tumor activity with average IC50 of 174.7 nM.
In Vivo

BET-IN-14 (Compound 171) (50 and 100 mg/kg, p.o., qd) inhibits tumor growth in MV-4-11 xenograft[1]。

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

Animal Model: Human MV-4-11 xenografts in Balb/c nude mice[1]
Dosage: 50 and 100 mg/kg
Administration: p.o., qd
Result: Inhibited tumor growth by 60.36%.
Molecular Weight

527.66

Formula

C30H37N7O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=CC=C(N2C(C3=CC(N(C4CCCC4)[C@H](C)C(N5C)=O)=C5C=C3)=NC(C(N6CCN(C)CC6)=O)=N2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (189.52 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 1.8952 mL 9.4758 mL 18.9516 mL
5 mM 0.3790 mL 1.8952 mL 3.7903 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; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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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: 2.5 mg/mL (4.74 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.74 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation
References

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; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8952 mL 9.4758 mL 18.9516 mL 47.3790 mL
5 mM 0.3790 mL 1.8952 mL 3.7903 mL 9.4758 mL
10 mM 0.1895 mL 0.9476 mL 1.8952 mL 4.7379 mL
15 mM 0.1263 mL 0.6317 mL 1.2634 mL 3.1586 mL
20 mM 0.0948 mL 0.4738 mL 0.9476 mL 2.3689 mL
25 mM 0.0758 mL 0.3790 mL 0.7581 mL 1.8952 mL
30 mM 0.0632 mL 0.3159 mL 0.6317 mL 1.5793 mL
40 mM 0.0474 mL 0.2369 mL 0.4738 mL 1.1845 mL
50 mM 0.0379 mL 0.1895 mL 0.3790 mL 0.9476 mL
60 mM 0.0316 mL 0.1579 mL 0.3159 mL 0.7896 mL
80 mM 0.0237 mL 0.1184 mL 0.2369 mL 0.5922 mL
100 mM 0.0190 mL 0.0948 mL 0.1895 mL 0.4738 mL
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BET-IN-14 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:

BET-IN-142243669-93-2Epigenetic Reader DomainCancerMM.1STy-82MV-4-11KG-1Inhibitorinhibitorinhibit

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