2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FLT3 Btk Apoptosis
  4. Luxeptinib

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.

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

Luxeptinib Chemical Structure

Luxeptinib Chemical Structure

CAS No. : 1616428-23-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 600 In-stock
25 mg USD 1150 In-stock
50 mg USD 1800 In-stock
100 mg USD 2950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Luxeptinib Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4].

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.

Luxeptinib Related Antibodies

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
Molecular Weight

495.43

Formula

C25H17F4N5O2
CAS No.
Appearance

Solid

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
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 : 50 mg/mL (100.92 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 2.0184 mL 10.0922 mL 20.1845 mL
5 mM 0.4037 mL 2.0184 mL 4.0369 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
×
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    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.

    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.
  • 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.

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

Purity: 99.30%

COA (254 KB) HNMR (299 KB) LCMS (108 KB)

Handling Instructions (2659 KB)
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 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
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Luxeptinib 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:

Luxeptinib1616428-23-9CG-806CG806CG 806FLT3BtkApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Bruton tyrosine kinasefirst-in-classnon-covalentmyeloidleukemialymphocytic\Inhibitorinhibitorinhibit

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