DT2216 | BCL-XL PROTAC | Probechem Biochemicals

Chemical Structure : DT2216

CAS No.: 2365172-42-3

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DT2216 (DT-2216)

货号: PC-38054Not For Human Use, Lab Use Only.

DT2216 (DT-2216) is a specific BCL-XL PROTAC by linking ABT263 to a VHL ligand (VHL-L), induces BCL-XL degradation in MOLT-4 T-ALL cells with DC50 of 63 nM.

规格	价格	库存
2 mg	￥1580	In stock
5 mg	￥2580	In stock
10 mg	￥3980	In stock
25 mg	￥5980	In stock
100 mg		Get quote

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生物&药学活性

DT2216 (DT-2216) is a specific BCL-XL PROTAC by linking ABT263 to a VHL ligand (VHL-L), induces BCL-XL degradation in MOLT-4 T-ALL cells with DC50 of 63 nM.
DT2216 exhibits improved antitumor potency (MOLT-4 cells EC50=52 nM) but reduced platelet toxicity by targeting BCL-XL to the VHL E3 ligase for degradation.
DT2216 degrades BCL-XL in a VHL- and proteasome-dependent manner.
DT2216 demonstrates increased antitumor activity of DT2216 in combination with other BCL-2 family protein inhibitors (ABT199 and S63845) and chemotherapy.
DT2216 sensitizes drug resistant tumor cells to chemotherapy in vivo.

物理化学性质&存储条件

分子量	1542.36
分子式	C77H96ClF3N10O10S4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(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-(phenylthio)butyl)piperazin-1-yl)-7-oxoheptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

参考文献

1. Khan S, et al. Nat Med. 2019 Dec;25(12):1938-1947.

2. Cancer Discov. 2020 Feb;10(2):174.

3. Thummuri D, et al. Mol Cancer Ther. 2022 Jan;21(1):184-192.

4. He Y, et al. J Hematol Oncol. 2020 Jul 16;13(1):95.

DT2216 (DT-2216)

生物&药学活性

物理化学性质&存储条件

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DT2216 (DT-2216)

生物&药学活性

物理化学性质&存储条件

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