DT-2216

99.10%

(2S,4R)-1-((S)-2-(7-(4-((R)-3-((4-(N-(4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoyl)sulfamoyl)-2-((trifluoromethyl)sulfonyl)phenyl)amino)-4-(pheny

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品牌：源叶(MedMol)

产品编号：S89374 一键复制产品信息

CAS号：2365172-42-3

分子式：C₇₇H₉₆ClF₃N₁₀O₁₀S₄

分子量：1542.36

别名：DT-2216; DT2216; DT 2216; DT2216 HCl, DT2216NC;

货号	规格	价格	上海	北京	珠海	重庆	武汉
S89374-5mg促销	99.10%	￥1250.00 ￥1000.00 S89374-5mg ￥1000.00 现货	6 6	-	-	-	-
S89374-10mg促销	99.10%	￥2050.00 ￥1640.00 S89374-10mg ￥1640.00 现货	2 2	-	-	-	-
S89374-25mg促销	99.10%	￥4500.00 ￥3600.00 S89374-25mg ￥3600.00 现货	2 2	-	-	-	-
S89374-100mg促销	≥98%	￥12000.00 ￥9600.00 S89374-100mg ￥9600.00 2-3天	0 货期：2-3天	-	-	-	-

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产品介绍参考文献(1篇) 质检证书(COA) 摩尔浓度计算器相关产品

产品描述：

DT2216 是一种基于PROTAC技术的 BCL-XL 的强效选择性降解剂。DT2216 抑制各种BCL-XL依赖性白血病和癌细胞，但对血小板的毒性较小

靶点：

BCL-XL;Apoptosis; LigandforE3Ligase; PROTACs

体外研究：

DT2216 is a BCL-XL proteolysis targeting chimera (PROTAC) that targets BCL-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation. DT2216 is more potent against various BCL-XL-dependent leukemia and cancer cells but significantly less toxic to platelets than ABT263 in vitro because VHL is poorly expressed in platelets.

体内研究：

In vivo, DT2216 effectively inhibits the growth of several xenograft tumors as a single agent or in combination with other chemotherapeutic agents, without causing significant thrombocytopenia

细胞实验：

Cell lines: MOLT-4, RS4;11, NCI-H146, MDA-MB-231, PC-3, HepG2, SW620, 786-O, WI-38, HEK 293T cells Concentrations: 0.1 μM, 0.3 μM Incubation Time: 24 h Method: MOLT-4 cells are seeded in 60 mm dishes (2.5 × 106 cells in 5 mL complete cell culture medium/dish), and then treated with indicated concentrations of DT2216 or ABT263 for 24 h. Cells are lysed in 1X cell lysis buffer by subjecting them to a freeze-thaw cycle in ice-ethanol bath or by 30 min incubation on ice.

动物实验：

Animal Models: female 5–6 week-old CB-17 SCID, CB-17 SCID-beige, NOD-SCID mice Dosages: 7.5 mg/kg, 15 mg/kg, 25 mg/kg Administration: IP

参考文献：

1. Sajid Khan, et al. A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity. Nat Med. 2019 Dec;25(12):1938-1947.

溶解性：

Soluble in DMSO、Ethanol

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	0.648 ml	3.242 ml	6.484 ml
5 mM	0.13 ml	0.648 ml	1.297 ml
10 mM	0.065 ml	0.324 ml	0.648 ml
50 mM	0.013 ml	0.065 ml	0.13 ml