化合物 AZD-5991|T10434|TargetMol

AZD-5991
2143061-81-6

￥2280 2mg 起订

￥2980 5mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 AZD-5991

英文名称：: AZD-5991

CAS号：: 2143061-81-6

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

产品类别：: 抑制剂

货号：: T10434

Product Introduction

Bioactivity

名称	AZD-5991
描述	AZD-5991 is a potent and selective Mcl-1 inhibitor (IC50: 0.7 nM in FRET assay; Kd: 0.17 nM in SPR assay).
体外活性	AZD-5991 is selective for Mcl-1 (IC50: 0.72?nM, Ki: 200?pM) vs. Bcl-2 (IC50: 20?μM, Ki: 6.8?μM), Bcl-xL (IC50: 36?μM, Ki: 18?μM), Bcl-w (IC50: 49?μM, Ki: 25?μM), and Bfl-1 (IC50: 24?μM, Ki: 12?μM). MOLP-8, MV4-11, and NCI-H23 cells are treated with AZD5991 (EC50: 0.033, 0.024, 0.19?μM, respectively). AZD5991 binds directly to Mcl-1 and induces rapid apoptosis in cancer cells by activating the Bak-dependent mitochondrial apoptotic pathway. AZD5991 reduces the levels of Mcl-1 protein in AZD5991-sensitive but not in AZD5991-resistant MM cell lines.
体内活性	A single intravenous (i.v.) dose of AZD5991 leads to a dose-dependent antitumor effect ranging from tumor growth inhibition (TGI) to tumor regression (TR). Ten days after treatment, AZD5991 shows 52% and 93% TGI at 10 and 30?mg/kg, respectively. At the same time point, AZD5991 at 60?mg/kg leads to 99% TR with no detectable tumors in 6 out of 7 mice, while complete TR is seen in 7 out of 7 mice in the 100?mg/kg dose group. AZD5991 also shows a dose-dependent duration of response with tumors in the 100?mg/kg group growing back later than those in the 60?mg/kg group. The magnitude of in vivo tumor efficacy is correlated with activation of caspase-3 in the tumor and concentration of AZD5991 in plasma. Treatment with AZD5991 was well tolerated at all dose levels with no significant bodyweight loss. A single dose of AZD5991 36 days after the first dose causes tumor regression in 4 out of 4 mice. In mice dosed with AZD5991 at 100?mg/kg on day 0 and day 1, tumors grow back later than those dosed with a single dose of AZD5991 at the same dose level.
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 25 mg/mL (37.19 mM), Sonication is recommended.
关键字	AZD 5991 \| AZD5991 \| AZD-5991
相关产品	Navitoclax \| Diphenyl disulfide \| Venetoclax \| Thymoquinone \| Gossypol (acetic acid) \| (S)-(+)-Ibuprofen \| Rasagiline \| Gossypol \| UMI-77 \| (E)-Ferulic acid \| Lisaftoclax \| Allethrin

AZD-5991|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

化合物 AZD-5991相关厂家报价

2143010-83-5AZD-5991 Racemate
上海嘉定区澄浏公路52号 VIP
2024-12-23
询价

AZD-9574
武汉铼辉生物科技有限公司 VIP
2024-12-05
询价

AZD-9291
成都克莱蒙医药科技有限公司 VIP
2024-12-17
询价

2143061-81-6AZD-5991
上海嘉定区澄浏公路52号 VIP
2024-12-23
询价

内容声明