CAS NO: | 2226521-65-7 |
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 |
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] |
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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 |
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溶解性数据 | In Vitro: DMSO : 8.33 mg/mL(19.44 mM;Need ultrasonic) 配制储备液
* 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。 |