製品番号: HY-135317

Emavusertib

(別名: CA-4948)

7 Cited Publications

カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Emavusertib is an orally active inhibitor for IRAK4 (IC₅₀=57 nM) and FLT3. Emavusertib inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib exhibits antitumor activity in mouse model

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.97%
CAS 番号: 1801344-14-8
分子式: C₂₄H₂₅N₇O₅
分子量:491.50

保管条件:

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

Emavusertib 構造式

CAS 番号: 1801344-14-8

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (7)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

IRAK4

57 nM (IC₅₀)

IRAK アイソフォーム固有の製品をすべて表示 :

NF-κB アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
OCI-Ly10	IC₅₀	1.5 μM Compound: 24; CA-4948	Growth inhibition of human OCI-LY10 harboring mutant MYD88 Growth inhibition of human OCI-LY10 harboring mutant MYD88	[PMID: 33335659]

体外実験

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.

体内実験

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.

臨床実験

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

化学情報

CAS 番号 1801344-14-8
性状 Solid
分子量 491.50
分子式 C₂₄H₂₅N₇O₅
Color Light yellow to green yellow
SMILES

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

CA-4948
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

Publications (7)

All In Vivo Efficacy StudyBio/Physico-chemical AssayCell Proliferation/Viability AssayIHCWB

Sort by:

Journal Impact Factor

Blood

Paralog-specific signaling by IRAK1/4 maintains MyD88-independent functions in MDS/AML. [Abstract]

2023 Sep 14;142(11):989-1007. PMID: 37172199

Emavusertib purchased from MedChemExpress. Usage Cited in: Blood. 2023 Sep 14;142(11):989-1007. [Abstract]

IC₅₀ curves for CA-4948 (Emavusertib) (0.01-10000 nM; 24 h) and PF-06650833 in an assay measuring NF-kB activity upon TLR2 stimulation with PAM3CSK4 in THP1 NF-kB reporter cells.

Emavusertib purchased from MedChemExpress. Usage Cited in: Blood. 2023 Sep 14;142(11):989-1007. [Abstract]

Immunoblots for phospho-IRAK1, total IRAK1, IRAK2, and IRAK4 in MDSL and AML (1714) treated for 24 hours with CA-4948 (Emavusertib) (10 μM). The results showed that treatment with CA-4948 resulted in increased IRAK1 phosphorylation.
Leukemia

Targeting of IRAK4 and GSPT1 enhances therapeutic efficacy in AML via c-Myc destabilization. [Abstract]

2025 Sep;39(9):2163-2173. PMID: 40670672

Emavusertib purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Sep;39(9):2163-2173. [Abstract]

Cell viability was determined in THP1 and HL60 cells cultured with 10 µM CA-4948 (Emavusertib) or in OCI-AML3 and K562 cultured with 1 µM CA-4948 or vehicle (n = 4) for 14 days and then treated with CC-885 (n = 4).

Emavusertib purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Sep;39(9):2163-2173. [Abstract]

Immunoblots for c-MYC in the patient-derived AML samples (AML1794, AML1714) cultured with CA-4948 (Emavusertib) (10 µM) or vehicle for 14 days and then treated with CC-885 (50 nM) for 4 h.
Cell Rep

Disruption of fibroblast MYD88 signaling promotes antitumor immunity in pancreatic ductal adenocarcinoma. [Abstract]

2025 Sep 24;44(10):116347. PMID: 41004339

Emavusertib purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Sep 24;44(10):116347. [Abstract]

Harvested tumor weights by treatment condition (n = 8 per condition).Tumor growth studies demonstrated statistically significant inhibition with both CA-4948 (Emavusertib) (50 mg/kg; oral gavage; once daily) alone and ICB alone.

Emavusertib purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Sep 24;44(10):116347. [Abstract]

H&E and trichrome staining of tumors by treatment condition (Emavusertib (50 mg/kg; oral gavage; once daily), ect.) at 10× magnification. The scale bar represents 100 μm.
Front Immunol

Activation of Toll-Like Receptor 7 Signaling Pathway in Primary Sjögren's Syndrome-Associated Thrombocytopenia. [Abstract]

2021 Mar 9:12:637659. PMID: 33767707
Curr Issues Mol Biol

FLT3 and IRAK4 Inhibitor Emavusertib in Combination with BH3-Mimetics in the Treatment of Acute Myeloid Leukemia. [Abstract]

2024 Mar 29;46(4):2946-2960. PMID: 38666914
bioRxiv

2026 Feb 3.
bioRxiv

2026 Jan 9.

溶剤 & 溶解度

体外:

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)

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

2.0346 mL

10.1729 mL

20.3459 mL

5 mM

0.4069 mL

2.0346 mL

4.0692 mL

10 mM

0.2035 mL

1.0173 mL

2.0346 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, 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.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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: ≥ 2.08 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.

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.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (4.23 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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (277 KB)
SDS (393 KB)
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COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[1]. Wiese MD, et al. Investigational IRAK-4 inhibitors for the treatment of rheumatoid arthritis. Expert Opin Investig Drugs. 2020 Apr 17:1-8. [Content Brief]

[2]. Guidetti F, et al. Targeting IRAK4 with Emavusertib in Lymphoma Models with Secondary Resistance to PI3K and BTK Inhibitors. J Clin Med. 2023 Jan 4;12(2):399. [Content Brief]

[3]. Parrondo RD, et al. IRAK-4 inhibition: emavusertib for the treatment of lymphoid and myeloid malignancies. Front Immunol. 2023 Oct 26;14:1239082. [Content Brief]

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, 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

Emavusertib

7 Cited Publications

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Emavusertib

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MedChemExpress（MCE）の使用を引用している文献 Emavusertib

IRAK アイソフォーム固有の製品をすべて表示

NF-κB アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (7)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Emavusertib 関連分類

HY-135317 関連分類