2. Epigenetics
  3. Epigenetic Reader Domain
  4. Ziftomenib

Ziftomenib (KO-539) is an orally active menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151).

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

Ziftomenib Chemical Structure

Ziftomenib Chemical Structure

CAS No. : 2134675-36-6

Size Price Stock Quantity
5 mg USD 920 In-stock
10 mg USD 1280 In-stock
50 mg USD 2400 In-stock
100 mg USD 3000 In-stock
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500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Ziftomenib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Ziftomenib

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Ziftomenib (KO-539) is an orally active menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151)[1].

In Vitro

The mixed-lineage leukemia (MLL) protein is a histone methyltransferase critical for the epigenetic regulation of gene transcription. Many acute leukemias, including acute myeloblastic leukemia (AML), acute lymphoblastic leukemia (ALL) and mixed-lineage leukemia (MLL), are characterized by the presence of chimeric MLL fusion proteins that result from chromosomal translocations of the MLL gene located at chromosome 11, band q23 (11q23). MLL fusion proteins lack the original histone methyltransferase activity of the C-terminus of MLL and gain the ability to regulate transcription of numerous oncogenes, including HOX and MEIS1, resulting in increased cell proliferation and decreased cell differentiation, ultimately leading to leukemogenesis[1].

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

Ziftomenib Related Antibodies
Clinical Trial
Molecular Weight

717.87

Formula

C33H42F3N9O2S2
CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

N#CC(N1C[C@@H](N2CCN(S(=O)(C)=O)CC2)C)=CC3=C1C=CC(CN4CCC(NC5=C(C=C(CC(F)(F)F)S6)C6=NC(NC)=N5)CC4)=C3C
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 (139.30 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 1.3930 mL 6.9650 mL 13.9301 mL
5 mM 0.2786 mL 1.3930 mL 2.7860 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
×
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: ≥ 2.08 mg/mL (2.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (2.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 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.
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 1.3930 mL 6.9650 mL 13.9301 mL 34.8252 mL
5 mM 0.2786 mL 1.3930 mL 2.7860 mL 6.9650 mL
10 mM 0.1393 mL 0.6965 mL 1.3930 mL 3.4825 mL
15 mM 0.0929 mL 0.4643 mL 0.9287 mL 2.3217 mL
20 mM 0.0697 mL 0.3483 mL 0.6965 mL 1.7413 mL
25 mM 0.0557 mL 0.2786 mL 0.5572 mL 1.3930 mL
30 mM 0.0464 mL 0.2322 mL 0.4643 mL 1.1608 mL
40 mM 0.0348 mL 0.1741 mL 0.3483 mL 0.8706 mL
50 mM 0.0279 mL 0.1393 mL 0.2786 mL 0.6965 mL
60 mM 0.0232 mL 0.1161 mL 0.2322 mL 0.5804 mL
80 mM 0.0174 mL 0.0871 mL 0.1741 mL 0.4353 mL
100 mM 0.0139 mL 0.0697 mL 0.1393 mL 0.3483 mL
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Ziftomenib 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:

Ziftomenib2134675-36-6KO-539KO539KO 539Epigenetic Reader DomainMeninantitumormixed-lineageleukemiaMLLInhibitorinhibitorinhibit

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