Desmorpholinyl Quizartinib-PEG2-COOH

• CAT Number: I045467
• CAS Number: 2292116-14-2
• Molecular Formula: C30H33N5O7S
• Molecular Weight: 607.68
• Purity: ≥95%
• Synonyms: 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]propanoic acid
• InChI: InChI=1S/C30H33N5O7S/c1-30(2,3)25-17-26(34-42-25)33-28(38)31-20-6-4-19(5-7-20)22-18-35-23-9-8-21(16-24(23)43-29(35)32-22)41-15-14-40-13-12-39-11-10-27(36)37/h4-9,16-18H,10-15H2,1-3H3,(H,36,37)(H2,31,33,34,38)
• InChIKey: BMRGZWDBDUKFLR-UHFFFAOYSA-N
• SMILES: CC(C)(C)C1=CC(=NO1)NC(=O)NC2=CC=C(C=C2)C3=CN4C5=C(C=C(C=C5)OCCOCCOCCC(=O)O)SC4=N3

Desmorpholinyl Quizartinib-PEG2-COOH incorporates a ligand for FLT-3, and a PEG-based PROTAC linker. Desmorpholinyl Quizartinib-PEG2-COOH can be used in the synthesis of PROTAC FLT-3 degrader 1 (HY-114323). PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM[1].

Reference

[1]. Burslem GM, et al. Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion. J Am Chem Soc. 2018 Dec 5;140(48):16428-16432.
 [Content Brief]