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MS 154

CAT: 0931-T41155Size: 5 mgDry Ice: NoHazardous: No
CAT#:0931-T41155Size:5 mg
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AVAILABILITY: InStock
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
2550393-21-8
Target
EGFR|||PROTACs|||Others
Related Pathways
PROTAC|||JAK/STAT signaling|||Tyrosine Kinase/Adaptors|||Angiogenesis|||Others
Bioactivity
MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib (Iressa) . MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioavailable in mice following ip administration.
Smiles
O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2OCCCCCCCCNC(CCN4CCN(CCCOC5=CC6=C(C=C5OC)N=CN=C6NC7=CC(Cl)=C(F)C=C7)CC4)=O
Molecular Formula
C46H54ClFN8O8
Molecular Weight
901.42
Shipping Conditions
Cool pack
Storage Temperature
-20°C

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