AZD4320 250mg

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Qiagen 凯杰 Biosharp Omega

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首页酶、辅酶及抑制剂MCE>

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商品介绍
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AZD4320 是 BH-3 的新型类似物，有效的 BCL2/BCLxL 的双重抑制剂。AZD4320 对于 KPUM-MS3，KPUM-UH1，和 STR-428 细胞系的 IC₅₀ 分别为 26 nM，17 nM，和 170 nM。

Description

AZD4320 is a novel BH3-mimicking dual BCL2/BCLxL inhibitor with IC₅₀s of 26 nM, 17 nM, and 170 nM for KPUM-MS3, KPUM-UH1, and STR-428 cells, respectively.

IC₅₀ & Target

BCL2

17 nM (IC₅₀, KPUM-UH1 cells)

BCLxL

17 nM (IC₅₀, KPUM-UH1 cells)

In Vitro

AZD4320 potently augments the antitumor effect of AZD5153 (Cat. No.: HY-100653A) in double expressing lymphoma (DEL)- and double hit lymphoma (DHL)-derived cell lines in a dose-dependent manner. AZD4320 shows mostly synergistic, and at least additive, growth inhibitory effects on DEL- and DHL derived cell lines, and profoundly increases cells undergoing apoptosis in all three cell lines^[1].

Solvent & Solubility

In Vitro:

10 mM in DMSO

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.0576 mL	5.2880 mL	10.5761 mL
5 mM	0.2115 mL	1.0576 mL	2.1152 mL
10 mM	0.1058 mL	0.5288 mL	1.0576 mL

* Please refer to the solubility information to select the appropriate solvent.

References

[1]. Takimoto-Shimomura T, et al. Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2. Invest New Drugs. 2018 Jun 21.

Cell Assay ^[1]	Two DEL-derived cell lines, KPUM-MS3 and KPUM-UH1, and a DHL-derived cell line, STR-428 are used. To examine the combinatory growth inhibitory effects of AZD4320, cells are treated with five concentrations (0.25, 0.5, 1.0, 2.0, 4.0×IC₅₀) for 72 h, and subjected to a modified MTT assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Takimoto-Shimomura T, et al. Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2. Invest New Drugs. 2018 Jun 21.

Cell Assay
^[1]

Two DEL-derived cell lines, KPUM-MS3 and KPUM-UH1, and a DHL-derived cell line, STR-428 are used. To examine the combinatory growth inhibitory effects of AZD4320, cells are treated with five concentrations (0.25, 0.5, 1.0, 2.0, 4.0×IC₅₀) for 72 h, and subjected to a modified MTT assay^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Takimoto-Shimomura T, et al. Dual targeting of bromodomain-containing 4 by AZD5153 and BCL2 by AZD4320 against B-cell lymphomas concomitantly overexpressing c-MYC and BCL2. Invest New Drugs. 2018 Jun 21.

Molecular Weight	945.53
Formula	C₄₅H₄₈ClF₃N₄O₇S₃
CAS No.	1357576-48-7
SMILES	O=C(NS(=O)(C1=CC=C(N[C@H](CCN(CCO)C)CSC2=CC=CC=C2)C(S(=O)(C(F)(F)F)=O)=C1)=O)C3=CC=C(N4CCC([C@H](C5=CC=CC=C5C6=CC=C(Cl)C=C6)O)CC4)C=C3
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping	Room temperature in continental US; may vary elsewhere