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INY-03-041
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。
INY-03-041图片
CAS NO:2503017-97-6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
INY-03-041 是一种有效的、高选择性的、基于 PROTAC 的泛-AKT降解剂,由ATP 竞争性AKT抑制剂Ipatasertib (HY-15186) 结合 Lenalidomide (HY-A0003,Cereblon配体)组成。INY-03-041 可抑制AKT1AKT2AKT3IC50分别为 2.0 nM,6.8 nM 和 3.5 nM。
生物活性

INY-03-041 is a potent, highly selective and PROTAC-based pan-AKTdegrader consisting of the ATP-competitiveAKTinhibitorIpatasertib(HY-15186) conjugated toLenalidomide(HY-A0003,Cereblonligand). INY-03-041 inhibitsAKT1,AKT2andAKT3withIC50s of 2.0, 6.8 and 3.5 nM, respectively[1].

IC50& Target[1]

Akt1

2.0 nM (IC50)

Akt3

3.5 nM (IC50)

Akt2

6.8 nM (IC50)

Cereblon

 

体外研究
(In Vitro)

INY-03-041 (10-1000 nM; 0-24 hours) induces potent degradation of all three AKT isoforms in MDA-MB-468 cells[1].
INY-03-041 exhibits potent in vitro inhibition of S6K1 (IC50=37.3 nM) and PKG1 (IC50= 33.2 nM)[1].
INY-03-041 displays enhanced anti-proliferative effects compared withIpatasertib(HY-15186) in MDA-MB-468 and HCC1937 cells[1].
INY-03-041 (250 nM, 12 h) promotes sustained AKT degradation and inhibition of downstream signaling effects for up to 96 h, even after compound washout[1].

Western Blot Analysis[1]

Cell Line:MDA-MB-468 cells
Concentration:10 nM, 50 nM, 100 nM, 250 nM, 500 nM, 1000 nM
Incubation Time:2 hours, 4 hours, 6 hours, 8 hours, 10 hours, 12 hours, 24 hours
Result:Induced potent degradation of all three AKT isoforms in a dose-dependent manner after a 12-h treatment, with maximal degradation observed between 100 and 250 nM. At concentrations of 500 nM and greater, AKT degradation is diminished. Treatment with 250 nM of INY-03-041 over time reveals partial degradation of all AKT isoforms within 4 h and progressive loss of AKT abundance out to 24 h.
分子量

798.41

性状

Solid

Formula

C44H56ClN7O5

CAS 号

2503017-97-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 115 mg/mL(144.04 mM;ultrasonic and warming and heat to 80℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.2525 mL6.2624 mL12.5249 mL
5 mM0.2505 mL1.2525 mL2.5050 mL
10 mM0.1252 mL0.6262 mL1.2525 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。