DT2216

CAS: 2365172-42-3 F: C77H96ClF3N10O10S4 W: 1542.36

DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effecti

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Bioactivity	DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. DT2216 is composed of the Bcl-2 family protein inhibitor Navitoclax (HY-10087), a linker, and a VHL E3 ubiquitin ligase (Red: Navitoclax; Blue: VHL ligand; Black: linker)[1].
Invitro	DT2216 (62.5、125 nM；72 小时) 可以杀死 MOLT-4 细胞[1]。 DT2216 (0.001-10 μM；72 小时) 对 MOLT-4 细胞具有高毒性，EC50 为 0.052 μM[1]。 DT2216 (0.1、0.3 μM；24 小时) 通过 caspase-3 介导的 BCL-2 同源拮抗剂杀伤 (BAK) 和 BCL-2 相关 X 蛋白 (BAX) 依赖性方式诱导细胞凋亡来杀死 MOLT-4 细胞 [1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> DT2216 相关抗体: Apoptosis Analysis[1] Cell Line:
In Vivo	DT2216 (腹腔注射；7.5、15 mg/kg；每周一次，持续 60 天) 以 15 mg/kg 剂量在抑制小鼠 MOLT-4 T-ALL 异种移植物生长方面比 7.5 mg/kg 更有效[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
CAS	2365172-42-3
Formula	C77H96ClF3N10O10S4
Molar Mass	1542.36
Appearance	固体
Transport	Room temperature in continental US; may vary elsewhere.
Storage	-20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Reference	[1]. Khan S, et al. A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity. Nat Med. 2019 Dec;25(12):1938-1947.