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Barasertib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Barasertib图片
CAS NO:722543-31-9
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
巴拉塞替
AZD1152
产品介绍
BaRasertib 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。

产品描述

AZD1152 is a pro-drug of Barasertib-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.

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

Administration of AZD1152 (25 mg/kg) alone markedly suppresses the growth of MOLM13 xenografts, confirmed by the observation of necrotic tissue with infiltration of phagocytic cells[1]. AZD1152 (25 mg/kg/day) treatment reduces xenograft levels such that they are slightly lower levels than after the first round of treatment, but this is not statistically significant indicating that residual cells might be more resistant to a second cycle of AZD1152[4]. In addition, AZD1152 (10-150 mg/kg/day) significantly inhibits the growth of a variety of human solid tumor xenografts, including colon, breast, and lung cancers, in a dose-dependent manner[2].

Cas No.

722543-31-9

分子式

C26H31FN7O6P

分子量

587.54

别名

巴拉塞替;AZD1152

储存和溶解度

DMSO:33 mg/mL (56.17 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years