基本信息 产品详情 公司简介 推荐产品
网站主页 AZD5991 AZD-5991
  • 2143061-81-6AZD-5991

2143061-81-6AZD-5991

AZD-5991
2143061-81-6
询价 1盒 起订
上海 更新日期:2024-12-23

上海一研生物科技有限公司

VIP3年
联系人:吴菲
电话:021-69985186拨打
手机:13611928337 拨打
邮箱:3427709316@qq.com

产品详情:

中文名称:
AZD-5991
英文名称:
AZD-5991
CAS号:
2143061-81-6
品牌:
一研
保存条件:
Store at -20°C
产品类别:
抑制剂
Cas:
2143061-81-6

产品属性:

产品名称

规格

CAS

型号

AZD-5991

0 mM * 1 mL in DMSO 5mg 10mg 50mg

2143061-81-6

EY-Y0165129

Cas No.2143061-81-6

别名 N/A

化学名 N/A

分子式 C35H34ClN5O3S2

AZD-5991.png

分子量 672.26

溶解度 DMSO : 41.67 mg/mL (61.98 mM);H2O : < 0.1 mg/mL (insoluble)

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述:
AZD-5991 is a potent and selective Mcl-1 inhibitor with an IC50 of 0.7 nM in FRET assay and a Kd of 0.17 nM in surface plasmon resonance (SPR) assay.

The selectivity of AZD-5991 is evaluated against pro-survival Bcl-2 family members using FRET assays. 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, most notably myeloma and acute myeloid leukemia, 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 further supporting the notion that activation of caspases by AZD5991 reduces Mcl-1 protein levels in AZD5991-sensitive cell lines[1].

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 (p<0.0001) 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 body weight 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[1].

[1]. Tron AE, et al. Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia. Nat Commun. 2018 Dec 17;9(1):5341.


2143061-81-6;C35H34ClN5O3S2;AZD-5991;

公司简介

上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业,公司自成立以来,秉承""全心全意服务于科研工作者""的企业理念,立足生物科技领域,运用生物技术和科研试剂,发展现代生物科技,为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品,服务生物科技领域的科学研究人员。 公司具有对普通货物、冷藏及冷冻仓库的存储、包装及运输能力。 公司将始终坚持信誉立业、以人为本、质量保证、诚信服务的宗旨,不断拼搏,开拓进取,与各界朋友携手共创美好未来。

成立日期 (11年)
注册资本 100
员工人数 50-100人
年营业额 ¥ 100万以内
经营模式 工厂,试剂
主营行业 生化试剂,抗体,细胞培养,分子生物学,免疫安全

AZD-5991相关厂家报价

  • AZD-9574
  • AZD-9574
  • 武汉铼辉生物科技有限公司 VIP
  • 2024-12-05
  • 询价
  • AZD-9291
  • AZD-9291
  • 成都克莱蒙医药科技有限公司 VIP
  • 2024-12-17
  • 询价
  • AZD-7648
  • AZD-7648
  • 上海安屹诺生物医药科技有限公司 VIP
  • 2024-12-05
  • ¥4000
内容声明
拨打电话 立即询价