Art. -Nr.: HY-153714

Zefamenib

(Synonyms: BN-104; BNM-1192; Menin-MLL inhibitor 27)

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Zefamenib (BN-104) is an effective selective brain membrane protein inhibitor with oral activity, and it's also a Menin inhibitor, it can block the Menin-MLL interaction and leads to the degradation of Menin protein. Zefamenib is a weak hERG inhibitor, with an IC₅₀ greater than 100 μM. Zefamenib has anti-tumor activity and can be used in cancer research, such as for acute myeloid leukemia.

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Reinheit: 99.95%
CAS. Nr.: 2938995-50-5
Formel: C₃₁H₃₅FN₈O₂
Molecular Weight:570.66

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Zefamenib Chemical Structure

CAS. Nr.: 2938995-50-5

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Preis

Verfügbarkeit

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

hERG

>100 μM (IC₅₀)

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In Vitro

Zefamenib (BN-104) inhibits the proliferation of leukemia cells, with IC₅₀ values of: MV-4-11 AF4 fusion (3.5 nM); MOLM13 AF9 fusion (12 nM); OCI-AML3 NPM1 mutant (11 nM)^[1].
Zefamenib (10 μM, 0-24 h) causes degradation of Menin protein in MV-4-11 cells ^[1].

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

Cell Viability Assay^[1]

Cell Line:

MV-4-11, MOLM13, OCI-AML3
Concentration:

0.0001, 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time:
Result:

Inhibited cell proliferation.

Western Blot Analysis^[1]

Cell Line:

MV-4-11
Concentration:

10 μM
Incubation Time:

2, 4, 6, 8, 24 h
Result:

Decreased expression of Menin protein.

In Vivo

Zefamenib (BN-104) (0-60 mg/kg, oral, twice a day, 21 days) inhibits tumor proliferation in a mouse model^[1].

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

Animal Model:

MV-4-11 xenograft mouse model^[1]
Dosage:

0, 10, 30, 60 mg/kg; twice a day; 21 days
Administration:

Oral
Result:

Inhibited tumor proliferation.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2938995-50-5
Appearance Solid
Molecular Weight 570.66
Formel C₃₁H₃₅FN₈O₂
Color White to off-white
SMILES

O=C([C@@H]1[C@]2([H])[C@](CCC2)([H])CN1)N3CCC4(CC3)CN(C5=NC=NN=C5OC6=C(C7=CN=CN=C7C8CC8)C=C(C=C6)F)C4
Synonyms

BN-104; BNM-1192; Menin-MLL inhibitor 27
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (175.24 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

1.7524 mL

8.7618 mL

17.5236 mL

5 mM

0.3505 mL

1.7524 mL

3.5047 mL

10 mM

0.1752 mL

0.8762 mL

1.7524 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. 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (4.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (280 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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]. Taishan Hu, et al. "Discovery of a novel menin-MLL inhibitor for potential treatment of MLLr leukemias and NPM1c AML." Cancer Research. Vol. 82. No. 12. 615 CHESTNUT ST, 17TH FLOOR, PHILADELPHIA, PA 19106-4404 USA: AMER ASSOC CANCER RESEARCH, 2022.

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

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	1.7524 mL	8.7618 mL	17.5236 mL	43.8089 mL
	5 mM	0.3505 mL	1.7524 mL	3.5047 mL	8.7618 mL
	10 mM	0.1752 mL	0.8762 mL	1.7524 mL	4.3809 mL
	15 mM	0.1168 mL	0.5841 mL	1.1682 mL	2.9206 mL
	20 mM	0.0876 mL	0.4381 mL	0.8762 mL	2.1904 mL
	25 mM	0.0701 mL	0.3505 mL	0.7009 mL	1.7524 mL
	30 mM	0.0584 mL	0.2921 mL	0.5841 mL	1.4603 mL
	40 mM	0.0438 mL	0.2190 mL	0.4381 mL	1.0952 mL
	50 mM	0.0350 mL	0.1752 mL	0.3505 mL	0.8762 mL
	60 mM	0.0292 mL	0.1460 mL	0.2921 mL	0.7301 mL
	80 mM	0.0219 mL	0.1095 mL	0.2190 mL	0.5476 mL
	100 mM	0.0175 mL	0.0876 mL	0.1752 mL	0.4381 mL

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Zefamenib

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Anti-Blood Cancer Compound Library

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Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zefamenib

Reprogramming Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Blood Cancer Compound Library

Neurodegenerative Disease-related Compound Library

Protein-protein Interaction Inhibitor Library

Potassium Channel Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Epigenetics Compound Library

Membrane Transporter/Ion Channel Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zefamenib Related Classifications

HY-153714 Related Classifications