Art. -Nr.: HY-139535

Luxeptinib

(Synonyms: CG-806)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells.

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Reinheit: 98.95%
CAS. Nr.: 1616428-23-9
Formel: C₂₅H₁₇F₄N₅O₂
Molecular Weight:495.43

Speicherung:

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

Luxeptinib Chemical Structure

CAS. Nr.: 1616428-23-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Pan-FLT3/Pan-BTK^[1]

In Vitro

Luxeptinib (MEC-1 CLL cells; 0.1~10 μM; 72 hours) inhibits cells proliferation with an IC₅₀ of 32 nM^[1].
? Luxeptinib inhibits BCR signaling-induced phosphorylation of BTK, PLCg2, AKT, ERK1/2, S6 ribosomal protein and strongly suppresses SYK phosphorylation in primary chronic lymphocytic leukemia (CLL) cells^[1]. Luxeptinib (MV4-11 cells; 500 pM; 1 hour) completely inhibits phosphorylation of FLT3 and STAT5^[2].

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

Cell Proliferation Assay^[1]

Cell Line:

MEC-1 CLL cells
Concentration:

0.1~10 µM
Incubation Time:

72 hours
Result:

Inhibited cells proliferation with an IC₅₀ of 32 nM.

Clinical Trial

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

Chemical Information

CAS. Nr. 1616428-23-9
Appearance Solid
Molecular Weight 495.43
Formel C₂₅H₁₇F₄N₅O₂
Color Light yellow to yellow
SMILES

O=C(NC1=C(F)C=C(F)C=C1F)NC2=CC(F)=C(C(C=CC(C3=NC(C)=CN3)=C45)=C5CNC4=O)C=C2
Synonyms

CG-806
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

Publications (1)

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Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (100.92 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

2.0184 mL

10.0922 mL

20.1845 mL

5 mM

0.4037 mL

2.0184 mL

4.0369 mL

10 mM

0.2018 mL

1.0092 mL

2.0184 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 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.05 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.20 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.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (4.20 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 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 (279 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)
- Korean - KR (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]. Ekaterina Kim MS, et al. CG-806, a First-in-Class Pan-FLT3/Pan-BTK Inhibitor, Exhibits Broad Signaling Inhibition in Chronic Lymphocytic Leukemia Cells. bloodjournal Blood blood (2019). 134 (Supplement_1) : 3051.

[2]. Abstract 44: CG′806, a first-in-class FLT3/BTK inhibitor, exhibits potent activity against AML patient samples with mutant or wild type FLT3, as well as other hematologic malignancy subtypes

[3]. Guopan Yu,et al.CG '806, a Novel Pan-FLT3/BTK Multi-Kinase Inhibitor, Induces Cell Cycle Arrest, Apoptosis or Autophagy in AML Cells Depending on FLT3 Mutation Status. Blood blood (2017).130 (Suppl_1) : 462

[4]. Aptose Biosciences to Present CG’806 Data at AACR Hematologic Malignancies Meeting

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	2.0184 mL	10.0922 mL	20.1845 mL	50.4612 mL
	5 mM	0.4037 mL	2.0184 mL	4.0369 mL	10.0922 mL
	10 mM	0.2018 mL	1.0092 mL	2.0184 mL	5.0461 mL
	15 mM	0.1346 mL	0.6728 mL	1.3456 mL	3.3641 mL
	20 mM	0.1009 mL	0.5046 mL	1.0092 mL	2.5231 mL
	25 mM	0.0807 mL	0.4037 mL	0.8074 mL	2.0184 mL
	30 mM	0.0673 mL	0.3364 mL	0.6728 mL	1.6820 mL
	40 mM	0.0505 mL	0.2523 mL	0.5046 mL	1.2615 mL
	50 mM	0.0404 mL	0.2018 mL	0.4037 mL	1.0092 mL
	60 mM	0.0336 mL	0.1682 mL	0.3364 mL	0.8410 mL
	80 mM	0.0252 mL	0.1262 mL	0.2523 mL	0.6308 mL
	100 mM	0.0202 mL	0.1009 mL	0.2018 mL	0.5046 mL

Keywords

Luxeptinib

1 Cited Publications

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Luxeptinib

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Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Membrane Protein-targeted Compound Library

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Cell Death Library

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Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Luxeptinib

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Luxeptinib

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Membrane Protein-targeted Compound Library

Autoimmune Disease Compound Library

Cytokine Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Luxeptinib

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Luxeptinib Related Classifications

HY-139535 Related Classifications