AZD-5991

An Mcl-1 inhibitor

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库存: 现货

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数量
5mg

￥3737.00

2990.00

- +
10mg

￥5875.00

4700.00

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50mg

￥17475.00

13980.00

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已选 0 种 0 瓶

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货号: ajce50736
CAS: 2143061-81-6
别名:
分子式: C35H34ClN5O3S2
分子量: 672.26
纯度: >98%
溶解度: DMSO : 41.67 mg/mL (61.98 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

AZD 5991 is an inhibitor of myeloid cell leukemia-1 (Mcl-1; IC₅₀ = 0.72 nM).¹ It is selective for Mcl-1 over Bcl-2, Bcl-xL, Bcl-W, and Bfl-1 (IC₅₀s = 20, 36, 49, and 24 ?M, respectively). AZD 5991 decreases the viability of MV4-11 acute myeloid leukemia (AML) and MOLP-8 multiple myeloma (MM) cells with EC₅₀ values of 24 and 33 nM, respectively. It disrupts formation of the Mcl-1-Bak complex and induces apoptosis in MOLP-8 cells when used at a concentration of 500 nM. AZD 5991 induces complete tumor regression in MV4-11 and MOLP-8 mouse xenograft models when administered at a single dose of 100 mg/kg.

1.Tron, A.E., Belmonte, M.A., Adam, A., et al.Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemiaNat. Commun.9(1)5341(2018)

Protocol

Animal experiment:

Mice and Rats[1]In mice, drugs (e.g., AZD5991; 10-100?mg/kg) are dosed intravenously in a volume of 5?mL/kg except for Venetoclax that is dosed orally in a volume of 10?mL/kg. One million MV4-11, five million MOLP-8, ten million NCI-H929 or five million OCI-AML3 cells are injected subcutaneously in the right flank of mice in a volume of 0.1?mL. In rats, AZD5991 (10-100?mg/kg) is dosed intravenously in a volume of 10?mL/kg. Ten million MV4-11 cells are injected subcutaneously in the right flank of rats in a volume of 0.1?mL. Tumor volumes (measured by caliper), animal body weight, and tumor condition are recorded twice weekly for the duration of the study. The tumor volume is calculated[1].

参考文献:

[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.