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BETd-246

Chemical Structure : BETd-246

CAS No.: 2140289-17-2

BETd-246 (BETd 246;BETd246)

Catalog No.: PC-60931Not For Human Use, Lab Use Only.

A potent, second-generation BET protein degrader that exhibits superior selectivity, potency and antitumor activity.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent, second-generation BET protein degrader that exhibits superior selectivity, potency and antitumor activity; completely and selectively depletes BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation; displays strong growth inhibition and apoptosis induction activity in TNBC cell lines with IC50 <1 uM, induces a rapid and time-dependent downregulation of MCL1 protein; decreases BET proteins in xenograft breast tumors and suppress tumor growth in vivo without causing weight loss.

Physicochemical Properties

M.Wt 946.035
Formula C48H55N11O10
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino)-7-(3,5-dimethylisoxazol-4-yl)-N-(3-(2-(2-(3-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)propoxy)ethoxy)ethoxy)propyl)-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide

References

1. Bai L, et al. Cancer Res. 2017 May 1;77(9):2476-2487.

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