Bioactivity | PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader for cyclin-dependent kinases (DC50 is 18.73 nM for CDK2) and the FMS-like tyrosine kinase 3 (FLT3). PROTAC FLT3/CDKs degrader-1 induces differentation of HL-60 (72.77% differentation at 6.25 nM), inhibits proliferation of AML cells, with IC50s of 2.9-37 nM. PROTAC FLT3/CDKs degrader-1 is potential for ameliorating acute myeloid leukemia. (Pink: ligand for target protein FLT3/CDKs ligand-1 (HY-161709); Black: linker (HY-W012935); Black: ligand for E3 ligase Thalidomide 5-fluoride (HY-W087383))[1] |
Formula | C40H42N12O5 |
Molar Mass | 770.84 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Barik S. Expression and biochemical properties of a protein serine/threonine phosphatase encoded by bacteriophage lambda. Proc Natl Acad Sci U S A. 1993 Nov 15;90(22):10633-7. |