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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $44 | In Stock | |
2 mg | $64 | In Stock | |
5 mg | $97 | In Stock | |
10 mg | $163 | In Stock | |
25 mg | $289 | In Stock | |
50 mg | $463 | In Stock | |
100 mg | $683 | In Stock | |
1 mL x 10 mM (in DMSO) | $163 | In Stock |
Description | 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. |
Targets&IC50 | EML4-ALK:59 nM(DC50)(NCI-H2228 cells), NPM-ALK:11 nM(DC50)(SU-DHL-1 cells), ALK:33 nM(SU-DHL-1 cells) |
In vitro | MS4078 effectively inhibits cancer cell proliferation by inducing ALK protein degradation via a cereblon and proteasome-dependent mechanism. In SU-DHL-1 cells, it shows an IC50 of 33 nM, and potently reduces ALK fusion protein levels, inhibits ALK auto-phosphorylation, and downstream STAT3 phosphorylation in a concentration-dependent manner. It specifically reduces NPM-ALK protein levels in SU-DHL-1 cells (DC50 of 11 nM) and EML4-ALK protein levels in NCI-H2228 cells (DC50 of 59 nM). |
Molecular Weight | 914.47 |
Formula | C45H52ClN9O8S |
Cas No. | 2229036-62-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 49 mg/mL (53.58 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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