产品
编 号：F622043
分子式：C24H25N7O5
分子量：491.5
分子式：C24H25N7O5
分子量：491.5
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1801344-14-8
产品详情
生物活性：
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.
体内研究：
Emavusertib (CA-4948) 在动物模型中表现出抗肿瘤活性，包括含有 MyD88 基因突变的肿瘤。Emavusertib 在 FLT3 野生型和 FLT3 突变型急性髓性白血病 (AML) 小鼠模型中显示出抗白血病活性。Emavusertib (25-150 mg/kg，口服，每日一次，连续 14 天)可诱导小鼠肿瘤生长抑制。Animal Model:Mice bearing OCI-LY10 tumors
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.
体外研究：
与 IRAK-1 相比，Emavusertib (CA-4948) 对 IRAK-4 的选择性高 500 多倍。Emavusertib 减少 TNF-α、IL-1β、IL-6 和 IL-8 从 TLR 刺激的 THP-1 细胞中释放，IC50 Emavusertib 相关抗体:
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.
体内研究：
Emavusertib (CA-4948) 在动物模型中表现出抗肿瘤活性，包括含有 MyD88 基因突变的肿瘤。Emavusertib 在 FLT3 野生型和 FLT3 突变型急性髓性白血病 (AML) 小鼠模型中显示出抗白血病活性。Emavusertib (25-150 mg/kg，口服，每日一次，连续 14 天)可诱导小鼠肿瘤生长抑制。Animal Model:Mice bearing OCI-LY10 tumors
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.
体外研究：
与 IRAK-1 相比，Emavusertib (CA-4948) 对 IRAK-4 的选择性高 500 多倍。Emavusertib 减少 TNF-α、IL-1β、IL-6 和 IL-8 从 TLR 刺激的 THP-1 细胞中释放，IC50 Emavusertib 相关抗体:
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