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PROTAC FLT-3 degrader 1 - CAS 2230826-81-8

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PROTAC FLT-3 degrader 1 is an FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction[1]. IC50: 0.6 nM (FLT-3 ITD).

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Molecular Formula

C52H61N9O9S2

Molecular Weight

1020.23

PROTAC FLT-3 degrader 1

- Specification
  - Solubility
    
    10 mM in DMSO
    
    Storage
    
    Please store the product under the recommended conditions in the Certificate of Analysis.
    
    Shipping
    
    Room temperature in continental US; may vary elsewhere
    
    Synonyms
    
    (2S,4R)-1-[(2S)-2-[3-[2-[2-[2-[4-[(5-tert-butyl-1,2-oxazol-3-yl)carbamoylamino]phenyl]imidazo[2,1-b][1,3]benzothiazol-6-yl]oxyethoxy]ethoxy]propanoylamino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
- Properties
  - InChI Key
    
    IKJBYQODYFQASC-YKCITUTQSA-N
    
    InChI
    
    InChI=1S/C52H61N9O9S2/c1-31-45(71-30-54-31)34-10-8-32(9-11-34)27-53-47(64)40-24-36(62)28-60(40)48(65)46(52(5,6)7)58-44(63)18-19-67-20-21-68-22-23-69-37-16-17-39-41(25-37)72-50-56-38(29-61(39)50)33-12-14-35(15-13-33)55-49(66)57-43-26-42(70-59-43)51(2,3)4/h8-17,25-26,29-30,36,40,46,62H,18-24,27-28H2,1-7H3,(H,53,64)(H,58,63)(H2,55,57,59,66)/t36-,40+,46-/m1/s1
    
    Canonical SMILES
    
    CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)CCOCCOCCOC4=CC5=C(C=C4)N6C=C(N=C6S5)C7=CC=C(C=C7)NC(=O)NC8=NOC(=C8)C(C)(C)C)O
- Reference Reading
  - 1. Sunitinib-based Proteolysis Targeting Chimeras (PROTACs) reduced the protein levels of FLT-3 and c-KIT in leukemia cell lines
    
    Jiadai Zhai, Chuang Li, Bingxia Sun, Sinan Wang, Yuting Cui, Qingzhi Gao, Feng Sang Bioorg Med Chem Lett. 2022 Dec 15;78:129041. doi: 10.1016/j.bmcl.2022.129041.Epub 2022 Nov 1.
    
    Proteolysis Targeting Chimeras (PROTACs) based on multi-target inhibitors have been reported several times recently. The advantages of PROTACs technology and the synergistic mechanism of multi-target drugs endow this class of protein degraders with special research significance. Herein, twelve new PROTACs based on Sunitinib and VHL-ligand were synthesized and evaluated for their in vitro anticancer activities. Among them, PROTACs 5 (IC50 = 2.9 ± 1.5 μM) exhibited the most significant antiproliferative activity against HL-60 cells. Western blot results showed that PROTAC 5 reduced the protein levels of FLT-3 and c-KIT in HL-60 cells, and induced the degradation of FLT-3 via the ubiquitin-proteasome system. Moreover, PROTACs 5 and 6 reduced the protein levels of FLT-3 in K562 cells. These results suggest that PROTAC 5 has the potential for further research, especially in combination with small molecule kinase inhibitors to study multidrug resistance of tyrosine kinase inhibitors in cancer treatment.

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