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CAS No.: 1801343-74-7

IRAK4-IN-7 Catalog No. CSN21077

Synonyms: CA-4948;CA4948-Analog;CA4948-Analog. Emavusertib

CA-4948 is a selective and potent IRAK4 inhibitor which can be used as a therapeutic agent for hematological cancers with dysregulated TLR/MYD88/IRAK4 signaling. CA-4948 exhibits favorable DMPK properties, oral bioavailability, and is well tolerated in mice. Furthermore, CA-4948 is previously shown to exhibit dose-dependent efficacy in ABC-DLBCL MYD88-L265P xenograft tumor models

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生物活性

实验方案

技术信息

生物活性

描述Interleukin-1 Receptor Associated Kinase-4 (IRAK-4) is a serine/threonine protein kinase belonging to tyrosine like kinase (TLK) family. It is one of the important signalling components downstream of IL-1/Toll family of receptors (IL-1R, IL-18R, IL-33R, Toll-like receptors) and plays a critical role in initiating innate immune response against foreign pathogens. Involved in Toll-like receptor (TLR) and IL-1R signaling pathways, IRAK-4 is rapidly recruited by MYD88 to the receptor-signaling complex upon TLR activation to form the Myddosome together with IRAK2.CA-4948, previously termed AU-4948, is a selective and potent IRAK4 inhibitor. According to data obtained from enzymatic assays, the inhibitory IC50 value of CA-4948 against human IRAK4 kinase is 37 nM. Moreover, CA-4948 showed high selectivity towards IRAK4 with kinase selectivity S35 score of 0.0343 at 1 μM. In vitro, CA-4948 inhibited ABC DLBCL OCI-LY10, SUDHL-2 and U2932 cells' viability with IC50 values of 3.58 μM, 7.86 μM and 10.42 μM, respectively. The treatment time was 72 h, and cell viability was determined by a CellTiter-Glo method. In western blot analysis of a DLBCL cell line during a 20 min TLR-agonist stimulation, CA-4948 suppressed the phosphorylation level of IKK-β, NF-kB p65, and JNK at the concentration of 10 μM^[1]. In ABC DLBCL OCI-LY3 xenograft model, CA-4948 administrated orally at the doses of 50 mg/kg or 150 mg/kg daily for more than 15 days resulted in tumor growth inhibition of 53% and 49%, respectively^[1].
作用机制CA-4948 is a potent and selective IRAK4 kinase inhibitor. According to docking mode study, CA-4948 anticipated to bind in ATP binding pocket close to gate-keeper Tyr262 residue in human IRAK4^[1].
动物研究
剂量
Mice: 37.5 mg/kg - 75 mg/kg^[1] (p.o., BID)

给药途径
p.o.
参考文献

动物研究
剂量	Mice: 37.5 mg/kg - 75 mg/kg^[1] (p.o., BID)
给药途径	p.o.

[1] CA-4948, First-in-Class Suppressor of the TLR Pathway

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3957 mL
- 11.9783 mL
- 23.9566 mL
- 5 mM
- 0.4791 mL
- 2.3957 mL
- 4.7913 mL
- 10 mM
- 0.2396 mL
- 1.1978 mL
- 2.3957 mL

技术信息

CAS号

1801343-74-7

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H19N7O3

运输

蓝冰

分子量

417.42

别名

CA-4948;CA4948-Analog;CA4948-Analog. Emavusertib

溶解度

DMSO	15.42 mg/mL (36.9 mM)
Water	insoluble

动物实验配方

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