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FM-381
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。
FM-381图片
CAS NO:2226521-65-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
FM-381 是有效,共价,可逆的JAK3抑制剂,靶向 Cys909 位点。FM-381 对 JAK3 的IC50值为127 pM,选择性分别比 JAK1,JAK2 和 TYK2 高 410,2700 和 3600 倍。
生物活性

FM-381 is a potent covalent reversible inhibitor ofJAK3targeting the unique Cys909. FM-381 has anIC50of 127 pM forJAK3, with 410, 2700 and 3600-fold selectivity overJAK1,JAK2andTYK2, respectively.

IC50& Target[1]

JAK3

127 pM (IC50)

体外研究
(In Vitro)

FM-381 is screened against a panel of 410 kinases at concentrations of 100 nM and 500 nM. FM-381 has no relevant effect on the activity of any tested kinases except JAK3 at a concentration of 100 nM. At 500 nM, FM-381 moderately inhibits 11 other kinases besides JAK3 with residual activities below 50%. FM-381 is found to be inactive in a selectivity panel of frequently hit BRDs (BRD4, BRPF, CECR, FALZ, TAF1, BRD9). FM-381 selectively inhibits JAK3 signaling in human CD4+T Cells. FM-381 shows an apparent EC50of 100 nM in a dose dependent BRET assay and blocks IL2 stimulated (JAK3/JAK1 dependent) STAT5 phosphorylation at 100 nM, but not JAK3 independent IL6 (JAK1/2/TYK dependent) stimulated STAT3 signalling in human CD4+T cells up to 1 μM[1].

分子量

428.49

性状

Solid

Formula

C24H24N6O2

CAS 号

2226521-65-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 8.33 mg/mL(19.44 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3338 mL11.6689 mL23.3378 mL
5 mM0.4668 mL2.3338 mL4.6676 mL
10 mM0.2334 mL1.1669 mL2.3338 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。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。