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Chemical Structure : Dual BCL-xL, BCL-2 degrader 753b
Catalog No.: PC-21928Not For Human Use, Lab Use Only.
Dual BCL-xL/BCL-2 degrader 753b (Compound 753b) is a highly potent dual BCL-xL and BCL-2 PROTAC degrader with DC50 of 6 nM and 48 nM for degrading BCL-xL and BCL-2 in 293T cells respectively.
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Dual BCL-xL/BCL-2 degrader 753b (Compound 753b) is a highly potent dual BCL-xL and BCL-2 PROTAC degrader with DC50 of 6 nM and 48 nM for degrading BCL-xL and BCL-2 in 293T cells respectively.
753b is a better PROTAC than DT2216 to induce the formation of the ternary complex.
753b degrades BCL-xL and BCL-2 in a VHL- and proteasome-dependent manner.
753b could substantially degrade WT and K20- and K87-only BCL-xL mutants, but not K16-only BCL-xL mutant.
753b is more potent than DT2216, ABT199 (a selective BCL-2 inhibitor) and ABT263 in killing Kasumi-1 cells by induction of apoptosis.
753b (5 mg/kg every four days) induced tumor regressions in H146 xenograft models.
| M.Wt | 1641.49 | |
| Formula | C82H105ClF3N11O11S4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Lv D, et al. Nat Commun. 2021 Nov 25;12(1):6896.
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