MS4078CAS号: 2229036-62-6分子式: C45H52ClN9O8S分子量: 914.47描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)
产品描述 | |
描述 |
MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK.
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纯度 |
98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
可溶性/溶解性 |
DMSO:49 mg/mL (53.58 mM)
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生物活性 | |
靶点 |
EML4-ALK:59 nM(DC50)(NCI-H2228 cells), NPM-ALK:11 nM(DC50)(SU-DHL-1 cells), ALK:33 nM(SU-DHL-1 cells)
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In vitro(体外研究) |
MS4078 effectively inhibits cancer cell proliferation. MS4078 induces ALK protein degradation via cereblon and proteasome dependent mechanism and potently inhibits proliferation of SU-DHL-1?cells with IC50 of 33 nM. MS4078 potently reduces the ALK fusion protein levels and inhibits the ALK auto-phosphorylation and down-steam STAT3 phosphorylation in both SU-DHL-1 and NCI-H2228?cells in a concentration-dependent manner. MS4078 reduces the NPM-ALK protein levels in SU-DHL-1 cells and the EML4-ALK protein levels in NCI-H2228 cells with DC50 of 11 nM and 59 nM, respectively.
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