Nampt degrader-2

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Nampt degrader-2

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

Nampt degrader-2 是一种荧光PROTAC，可有效降解NAMPT，IC₅₀为 41.9 nM。Nampt degrader-2 与 NAMPT 和 VHL 结合形成三元复合物，随后通过泛素-蛋白酶体系统 (UPS) 诱导 NAMPT 降解。Nampt degrader-2 导致 NAD⁺显着减少并发挥有效的抗肿瘤活性。

生物活性

Namptdegrader-2 is a fluorescentPROTAC, which efficiently degradesNAMPTwith anIC₅₀of 41.9 nM.Namptdegrader-2 binds toNAMPTand VHL to form a ternary complex and subsequently inducedNAMPTdegradation via ubiquitin-proteasome system (UPS).Namptdegrader-2 leads to significant reduction of NAD⁺and exerts potent antitumor activities^[1].

IC₅₀& Target^[1]

VHL	NAMPT 41.9 nM (IC₅₀)

体外研究
(In Vitro)

Nampt degrader-2 (Compound B4; 30 nM; 24 h) is able to degrade NAMPT with a DC₅₀value of 8.4 nM. Nampt degrader-2 enables the visualization of degradation in A2780 cells^[1].
Nampt degrader-2 (Compound B4) shows the best antitumor activity in suppression of the proliferation in A2780 cells (IC₅₀= 12.1 nM)^[1].

Western Blot Analysis^[1]

Cell Line:	A2780 cells
Concentration:	30 nM
Incubation Time:	24 h
Result:	Were able to degrade NAMPT in A2780 cells at the concentration of 30 nM.

体内研究
(In Vivo)

Nampt degrader-2 (Compound B4; 10-30 mg/kg; i.p; once a day; for 14 consecutive days) shows excellent antitumor effects in a dose-dependent manner. And Nampt degrader-2 significantly decreases the NAMPT levels in the tumors^[1].

Animal Model:	BALB/C nude female mice (4-5 weeks of age, 14-18 g) injected with A2780 cells^[1]
Dosage:	10 mg/kg, 30 mg/kg
Administration:	i.p; once a day; for 14 consecutive days
Result:	Achieved excellent antitumor effects in a dose-dependent manner.

分子量

1052.33

Formula

C₅₉H₇₃N₉O₇S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.