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Emavusertib {[allProObj[0].p_purity_real_show]}

貨號(hào)：A1152397 同義名： CA-4948

Emavusertib是一種具有口服活性和抗腫瘤活性的 IRAK4/FLT3 抑制劑。 Emavusertib 對(duì) IRAK4 的 IC50 為 57 nM。

Emavusertib 化學(xué)結(jié)構(gòu)
CAS號(hào)：1801344-14-8

Emavusertib 3D分子結(jié)構(gòu)
CAS號(hào)：1801344-14-8

規(guī)格	價(jià)格	會(huì)員價(jià)	庫(kù)存	數(shù)量
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Emavusertib 純度/質(zhì)量文件產(chǎn)品僅供科研

貨號(hào)：A1152397 標(biāo)準(zhǔn)純度： {[allProObj[0].p_purity_real_show]} 產(chǎn)品說(shuō)明書(shū)

批次查詢：批次純度: COA SDS NMR HPLC CNMR LC-MS

全球?qū)W術(shù)期刊中引用的產(chǎn)品: ? Nature, 2026. Ambeed. [ A111216 , A291101 , A169647 , A115820 , A113480 , A635338 , A139877 , A258659 ]; ? Adv. Mater., 2026, e11078. Ambeed. [ A1680754 ]; ? Adv. Mater., 2026, e17774. Ambeed. [ A551995 ]; ? Cell. Mol. Immunol., 2026. Ambeed. [ A145872 , A614767 , A136097 ]; ? ACS Nano, 2026, 20(2): 2200-2210. Ambeed. [ A232266 ]; 更多 >

Emavusertib 生物活性

描述

Interleukin-1 receptor-associated kinase 4 (IRAK4) is the most upstream kinase in Toll/Interleukin-1 receptor (TIR) signaling^[2]. In the chronic ethanol-induced liver injury mouse model, hepatic inflammation and hepatocellular damage were attenuated in Irak4 KI mice. IRAK4 kinase activity promotes expression of acute phase proteins in response to ethanol exposure, including C-reactive protein and serum amyloid A1 (SAA1). SAA1 and IL-1β synergistically exacerbate ethanol-induced cell death ex vivo. Pharmacological blockage of IRAK4 kinase abrogated ethanol-induced liver injury, inflammation, steatosis, as well as acute phase gene expression and protein production in mice^[3]. IRAK4 inhibition significantly abrogates colitis-induced neoplasm in APCMin/+ mice, and bone marrow transplant experiments showed an essential role of IRAK4 in immune cells during neoplastic progression^[4]. Emavusertib (CA-4948) is a potent IRAK4/FLT3 inhibtor with anti-tumor activity^[5]. CA-4948, demonstrated good cellular activity in ABC DLBCL and AML cell lines. Inhibition of TLR signaling leading to decreased IL-6 levels was also observed in whole blood assays. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation. CA-4948 was well tolerated in toxicity studies in both mouse and dog at efficacious exposure. The overall profile of CA-4948 prompted us to select it as a clinical candidate for evaluation in patients with relapsed or refractory hematologic malignancies including non-Hodgkin lymphoma and acute myeloid leukemia^[1].

Emavusertib 細(xì)胞實(shí)驗(yàn)

Cell Line Karpas1718 SKM-1 OCI-AML3 ML-2 VL51 MOLM-13	Concentration	Treated Time	Description	References
Karpas1718	3.72 μM (IC50)	72 hours	To evaluate the antiproliferative activity of Emavusertib as a single agent in MYD88 L265P-mutated MZL cell lines. Results showed that Karpas1718 cells were most sensitive to Emavusertib with an IC50 of 3.72 μM.	J Clin Med. 2023 Jan 4;12(2):399
SKM-1	50-250 nM	20 hours	increased cell viability	Curr Issues Mol Biol. 2024 Mar 29;46(4):2946-2960
OCI-AML3	50-250 nM	20 hours	increased cell viability	Curr Issues Mol Biol. 2024 Mar 29;46(4):2946-2960
ML-2	50-250 nM	20 hours	increased cell viability	Curr Issues Mol Biol. 2024 Mar 29;46(4):2946-2960
VL51	21-38 μM (IC50)	72 hours	To evaluate the antiproliferative activity of Emavusertib as a single agent in VL51 cell line and its derivatives. Results showed that VL51 cells and their derivatives were less sensitive to Emavusertib with IC50 values ranging from 21-38 μM.	J Clin Med. 2023 Jan 4;12(2):399
MOLM-13	50-250 nM	20 hours	induced cell cycle arrest, apoptosis and cell death	Curr Issues Mol Biol. 2024 Mar 29;46(4):2946-2960

Emavusertib 動(dòng)物實(shí)驗(yàn)

Species NSG mice	Animal Model MDS patient-derived xenograft model	Administration	Dosage	Frequency	Description	References
NSG mice	MDS patient-derived xenograft model	Oral	12.5 mg/kg/d	5 times a week for 3-4 weeks	To evaluate the effect of IRAK4 inhibitor CA-4948 on MDS clone growth. Results showed that CA-4948 significantly reduced MDS clone growth.	Elife. 2022 Aug 30;11:e78136

Emavusertib 參考文獻(xiàn)

[1]Bhumireddy A . Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies. Chemistry Letters, 2020, 11(12).

[2] William T McElroy. Interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitors: an updated patent review (2016-2018). Expert Opin Ther Pat. 2019 Apr;29(4):243-259.

[3]Han Wang,et al. Inhibition of IRAK4 kinase activity improves ethanol-induced liver injury in mice. J Hepatol. 2020 Dec;73(6):1470-1481.

[4]Qiong Li,et al. IRAK4 mediates colitis-induced tumorigenesis and chemoresistance in colorectal cancer. JCI Insight. 2019 Oct 3;4(19):e130867.

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

Emavusertib 實(shí)驗(yàn)方案

計(jì)算器

存儲(chǔ)液制備

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.17mL

2.03mL

1.02mL

20.35mL

4.07mL

2.03mL

Emavusertib 技術(shù)信息

CAS號(hào)	1801344-14-8
分子式	C₂₄H₂₅N₇O₅
分子量	491.5
SMILES Code	O=C(C1=COC(C2=CC(C)=NC=C2)=N1)NC3=C(N4C[C@H](O)CC4)N=C5C(OC(N6CCOCC6)=N5)=C3
MDL No.	MFCD32693907

別名	CA-4948
運(yùn)輸	藍(lán)冰
InChI Key	SJHNWSAWWOAWJH-MRXNPFEDSA-N
Pubchem ID	118224491

存儲(chǔ)條件

In solvent -20°C: 3-6個(gè)月 -80°C: 12個(gè)月

Pure form Sealed in dry, 2-8°C

溶解方案

細(xì)胞實(shí)驗(yàn)：

DMSO: 50 mg/mL(101.73 mM)，配合低頻超聲助溶，注意：DMSO長(zhǎng)時(shí)間開(kāi)封后，會(huì)吸水并導(dǎo)致溶解能力下降，請(qǐng)避免使用長(zhǎng)期開(kāi)封的DMSO

動(dòng)物實(shí)驗(yàn)：請(qǐng)根據(jù)您的動(dòng)物給藥指南選擇適當(dāng)?shù)娜芙夥桨浮?/a>
以下溶解方案都請(qǐng)先按照體外實(shí)驗(yàn)的方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百分比是指該溶劑在終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

方案二

方案三

Emavusertib {[allProObj[0].p_purity_real_show]}

Emavusertib 純度/質(zhì)量文件產(chǎn)品僅供科研

全球?qū)W術(shù)期刊中引用的產(chǎn)品

Emavusertib 質(zhì)控信息

Emavusertib 生物活性

Emavusertib 細(xì)胞實(shí)驗(yàn)

Emavusertib 動(dòng)物實(shí)驗(yàn)

Emavusertib 參考文獻(xiàn)

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Emavusertib {[allProObj[0].p_purity_real_show]}

Emavusertib 純度/質(zhì)量文件 產(chǎn)品僅供科研

全球?qū)W術(shù)期刊中引用的產(chǎn)品

Emavusertib 質(zhì)控信息

Emavusertib 生物活性

Emavusertib 細(xì)胞實(shí)驗(yàn)

Emavusertib 動(dòng)物實(shí)驗(yàn)

Emavusertib 參考文獻(xiàn)

Emavusertib 實(shí)驗(yàn)方案

Emavusertib 技術(shù)信息

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總藥量計(jì)算器

工作液計(jì)算器

細(xì)胞研究

臨床研究

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