2. Immunology/Inflammation Protein Tyrosine Kinase/RTK Apoptosis
  3. IRAK FLT3 Apoptosis
  4. Emavusertib

Emavusertib  (Synonyms: CA-4948)

Cat. No.: HY-135317 Purity: 99.96%
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Emavusertib (CA-4948) is a selective, potent and orally active IRAK4/FLT3 inhibitor. Emavusertib has an IC50 of 57 nM for IRAK4 in a FRET kinase assay. Emavusertib shows anti-tumor activity.

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

Emavusertib Chemical Structure

Emavusertib Chemical Structure

CAS No. : 1801344-14-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 95 In-stock
Solution
10 mM * 1 mL in DMSO USD 95 In-stock
Solid
5 mg USD 88 In-stock
10 mg USD 110 In-stock
25 mg USD 220 In-stock
50 mg USD 400 In-stock
100 mg USD 680 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 2 publication(s) in Google Scholar

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Emavusertib Related Antibodies

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IRAK1 IRAK4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Emavusertib (CA-4948) is a selective, potent and orally active IRAK4/FLT3 inhibitor. Emavusertib has an IC50 of 57 nM for IRAK4 in a FRET kinase assay. Emavusertib shows anti-tumor activity[1][2][3].

IC50 & Target[1]

IRAK4

57 nM (IC50)

In Vitro

Emavusertib (CA-4948) is over 500-fold more selective for IRAK-4 compared to IRAK-1. Emavusertib reduces TNF-α, IL-1β, IL-6 and IL-8 release from TLR-Stimulated THP-1 Cells with an IC50 <250 nM. Emavusertib also has antiproliferative activity due to inhibition of receptor-type tyrosine-protein kinase FLT3[1].
Emavusertib exhibits >350-fold higher binding affinity for IRAK-4 than that observed for IRAKs 1, 2 and 3[3].
Emavusertib (10 μM, 72 h) decreases the percentage of proliferating cells and induces a moderate increase in the sub-G0 fraction in marginal zone lymphomas (MZL) cell lines[3].
Emavusertib (10 μM, 72 h) induces a significant increase in the apoptotic cell population of MZL cells, particularly when combined with Ibrutinib (HY-10997) compared to ibrutinib and emavusertib alone[3].

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

Emavusertib Related Antibodies
In Vivo

Emavusertib (CA-4948) shows anti-tumor activity in animal models including tumors containing MyD88 gene mutations. Emavusertib shows antileukemic activity in mouse models of FLT3 wild-type and FLT3 mutated acute myeloid leukemia (AML)[1].
Emavusertib (25-150 mg/kg, Orally, once daily, for 14 consecutive days) induces tumor growth inhibition in mice[3].

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

Animal Model: Mice bearing OCI-LY10 tumors[3]
Dosage: 25, 50, or 150 mg/kg (once daily), 12.5, 25, or 50 mg/kg (twice daily)
Administration: Orally, once daily or twice daily, for 14 consecutive days
Result: Induced tumor growth inhibition. Emavusertib administered as a twice-daily divided dose was equivalent to the corresponding once-daily dose with regards to antitumor activity, i.e., 12.5 mg/kg BID versus 25 mg/kg QD.
Clinical Trial
Molecular Weight

491.50

Formula

C24H25N7O5
CAS No.
Appearance

Solid

SMILES

O=C(C1=COC(C2=CC(C)=NC=C2)=N1)NC3=C(N4C[C@H](O)CC4)N=C5C(OC(N6CCOCC6)=N5)=C3
Shipping

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

DMSO : 50 mg/mL (101.73 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 2.0346 mL 10.1729 mL 20.3459 mL
5 mM 0.4069 mL 2.0346 mL 4.0692 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.23 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% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (4.23 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 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 (20.8 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

Purity: 99.96%

COA (251 KB) HNMR (292 KB) LCMS (266 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0346 mL 10.1729 mL 20.3459 mL 50.8647 mL
5 mM 0.4069 mL 2.0346 mL 4.0692 mL 10.1729 mL
10 mM 0.2035 mL 1.0173 mL 2.0346 mL 5.0865 mL
15 mM 0.1356 mL 0.6782 mL 1.3564 mL 3.3910 mL
20 mM 0.1017 mL 0.5086 mL 1.0173 mL 2.5432 mL
25 mM 0.0814 mL 0.4069 mL 0.8138 mL 2.0346 mL
30 mM 0.0678 mL 0.3391 mL 0.6782 mL 1.6955 mL
40 mM 0.0509 mL 0.2543 mL 0.5086 mL 1.2716 mL
50 mM 0.0407 mL 0.2035 mL 0.4069 mL 1.0173 mL
60 mM 0.0339 mL 0.1695 mL 0.3391 mL 0.8477 mL
80 mM 0.0254 mL 0.1272 mL 0.2543 mL 0.6358 mL
100 mM 0.0203 mL 0.1017 mL 0.2035 mL 0.5086 mL
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Emavusertib 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:

Emavusertib1801344-14-8CA-4948CA4948CA 4948IRAKFLT3ApoptosisInterleukin-1 receptor associated kinaseIL-1R associated kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3inflammationMyd88rheumatoidarthritisTollIL-1RlymphomaInhibitorinhibitorinhibit

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