Nexatoclax | Bcl-2/xL inhibitor | Probechem Biochemicals

Chemical Structure : Nexatoclax

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Nexatoclax (LP-118, LP118)

货号: PC-26343Not For Human Use, Lab Use Only.

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100 mg		Get quote

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生物&药学活性

Nexatoclax (LP-118) is a potent small molecule inhibitor of Bcl-2 and Bcl-xL (IC50=10.1 nM), more potent than venetoclax and with added advantage of selectively binding to Bcl-xL while minimizing the platelet toxicity.
Nexatoclax (LP-118) shows IC50 of 0.5 nM for naive CLL cells, more sensitive to LP-118 than venetoclax and navitoclax.
Nexatoclax (LP-118) has IC50 of 20 nM for RS4; 11 cells harboring the Bcl-2 Gly101Val mutation.
Nexatoclax (LP-118) (100 mpk, oral gavage, daily) significantly decreases overall tumor growth and increases survival in RS4; 11 xenograft model.

物理化学性质&存储条件

分子量	925.50
分子式	C47H53ClN8O8S
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	(S)-N-((4-(((1,4-dioxan-2-yl)methyl)amino)-3-nitrophenyl)sulfonyl)-4-(4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-2-(3,4-dihydro-2H-pyrrolo[3',2':5,6]pyrido[2,3-b][1,4]oxazepin-1(7H)-yl)benzamide

参考文献

1. Patent WO2021173523 A1.

2. Patent WO2021066873 A1.

3. Janani Ravikrishnan, et al. Blood (2021) 138 (Supplement 1): 679.

Nexatoclax (LP-118, LP118)

生物&药学活性

物理化学性质&存储条件

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Nexatoclax (LP-118, LP118)

生物&药学活性

物理化学性质&存储条件

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