产品
编 号：F280124
分子式：C45H52ClN9O8S
分子量：914.47
分子式：C45H52ClN9O8S
分子量：914.47
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 2229036-62-6
产品详情
生物活性：
MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19?nM for binding affinity to ALK.
体外研究：
MS4078 effectively inhibits cancer cell proliferation. MS4078 (10-3, 10-2.5, 10-2, 10-1.5, 10-1, 10-0.5, 1 μM; 3 days) concentration-dependently inhibits proliferation of SU-DHL-1?cells with an IC50?of?33±1??nM. In comparison with SU-DHL-1?cells, the proliferation of NCI-H2228?cells is less sensitive to MS4078(10-2, 10-1.5, 10-1, 10-0.5, 1, 100.5 μM; 3 days).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. In SU-DHL-1?cells, MS4078 reduces the NPM-ALK protein levels with impressive DC50 (50% degradation) value of?11±2?nM after 16-hour treatment. Over 90% of inhibition of both ALK Y1507 and STAT3 Y705 phosphorylation is achieved at the 100?nM concentration. In NCI-H2228?cells, MS4078 reduces the EML4-ALK protein levels with similar DC50 value of?59?±?16?nM after 16-hour treatment.At the 100?nM concentration, NCI-H2228?cells reduces more than 90% of EML4-ALK protein levels.
MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19?nM for binding affinity to ALK.
体外研究：
MS4078 effectively inhibits cancer cell proliferation. MS4078 (10-3, 10-2.5, 10-2, 10-1.5, 10-1, 10-0.5, 1 μM; 3 days) concentration-dependently inhibits proliferation of SU-DHL-1?cells with an IC50?of?33±1??nM. In comparison with SU-DHL-1?cells, the proliferation of NCI-H2228?cells is less sensitive to MS4078(10-2, 10-1.5, 10-1, 10-0.5, 1, 100.5 μM; 3 days).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. In SU-DHL-1?cells, MS4078 reduces the NPM-ALK protein levels with impressive DC50 (50% degradation) value of?11±2?nM after 16-hour treatment. Over 90% of inhibition of both ALK Y1507 and STAT3 Y705 phosphorylation is achieved at the 100?nM concentration. In NCI-H2228?cells, MS4078 reduces the EML4-ALK protein levels with similar DC50 value of?59?±?16?nM after 16-hour treatment.At the 100?nM concentration, NCI-H2228?cells reduces more than 90% of EML4-ALK protein levels.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备