巴拉塞替 T14371

Product Introduction
Bioactivity


英文名: Barasertib

描述: Barasertib (AZD1152) 是 Barasertib-hQPA 的前体药物，在癌细胞中诱导生长停滞和凋亡。它是高度选择性的Aurora B 抑制剂，IC50值为 0.37 nM。

体外活性: AZD1152 inhibits the proliferation of hematopoietic malignant cells such as HL-60, NB4, MOLM13, PALL-1, PALL-2, MV4-11, EOL-1, THP-1, and K562 cells with IC50 of 3-40 nM, displaying appr 100-fold potency than another Aurora kinase inhibitor ZM334739 which has IC50 of 3-30 μM and it also inhibits the clonogenic growth of MOLM13 and MV4-11 cells with IC50 of 1 nM and 2.8 nM, respectively, as well as the freshly isolated imatinib-resistant leukemia cells with IC50 values of 1-3 nM, more significantly compared with bone marrow mononuclear cells with IC50 values of >10 nM. AZD1152 displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 μM. AZD1152 causes significant accumulation of cells with 4N/8N DNA content in KMS12 and U266 and induces apoptosis in KMS18 and U266. AZD1152 has even less activity against 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. AZD1152 induces accumulation of cells with 4N/8N DNA content, followed by apoptosis in a dose- and time-dependent manner[1]. AZD1152 in combination with DEX, has negative effects on cell viability in comparison with single agent in PMI8226, KMS11 and U266[3].

体内活性: 给予Barasertib（25mg/kg）单独使用显著抑制MOLM13异种移植瘤的生长，通过观察到含有吞噬细胞的坏死组织得到确认[1]。Barasertib（25mg/kg/天）治疗使异种移植瘤水平降低，虽然与第一轮治疗后的水平略有下降，但这种下降并不具有统计学意义，表明残余细胞可能对Barasertib的第二轮治疗更具抵抗性[4]。此外，Barasertib（10-150mg/kg/天）以剂量依赖性的方式显著抑制多种人类实体瘤异种移植瘤的生长，包括结肠癌、乳腺癌和肺癌[2]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 33 mg/mL (56.17 mM)


关键字: breast | cancer | colon | Aurora Kinase | Inhibitor | AZD 1152 | Barasertib | leukemia | lung | inhibit | Apoptosis | AZD-1152

相关产品: PF-3758309 hydrochloride | SCFSkp2-IN-2 | K-Ras(G12C) inhibitor 12 | Rapanone | Polyphyllin VI | Thrombospondin-1 (1016-1023) (human, bovine, mouse) | Anticancer agent 106 | Isatuximab | Penicillic acid | Buparlisib

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途