常用名：MS4078

产品描述：

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.

靶点活性 NPM-ALK:11 nM(DC50)(SU-DHL-1 cells), ALK:33 nM(SU-DHL-1 cells), EML4-ALK:59 nM(DC50)(NCI-H2228 cells)

体外活性 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.

分子量 914.47

分子式 C45H52ClN9O8S

CAS No. 2229036-62-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 49 mg/mL (53.58 mM), Sonication is recommended.

PROteolysis TArgeting Chimeras (PROTACs) 通过将靶蛋白和 E3 连接酶结合起来，从而“劫持”细胞的泛素-蛋白酶体系统（UPS）来实现蛋白质的降解。由于 PROTACs 只需具有高选择性地结合其靶标（而不是抑制靶蛋白的酶活性），目前有许多努力将先前无效的抑制剂分子改造为 PROTACs，用作下一代药物。

产地：西安

用途：科研！

厂家：西安齐岳生物科技有限公司

温馨提示：仅用于科研，不能用于人体实验！

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