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PROTAK™ BETd-260 (ZBC 260)
$1080/ 5mg
Specification
QuantityTotal: $1080
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Product Information
CAS No.2093388-62-4
Purity>98.00%
FormulaC43H46N10O6
M.W.798.89
SolubilityDMSO : 25 mg/mL (31.29 mM; Need ultrasonic);H2O : < 0.1 mg/mL (insoluble)
Storage/StabilityStore at -20°C
BackgroundBETd-260 is a potent BET degrader based on PROTAC technology, with an IC50 of 30 pM against BRD4 protein in RS4;11 leukemia cell line.BETd-260 is a potent BET degrader based on PROTAC technology, with an IC50 of 30 pM for BRD4 protein in RS4;11 leukemia cell line. BETd-260 (ZBC260; Compound 23) shows inhibitory activity against the growth of RS4;11 leukemia cells and MOLM-13 cells with IC50s of 51 pM and 2.2 nM, respectively, and induces apoptosis in both RS4;11 and MOLM-13 cell lines at 3-10 nM.BETd-260 (5 mg/kg, i.v., every other day, thrice a week for 3 weeks) causes rapid tumor regression with a maximum of >90% regression in mice bearing RS4;11 xenograft tumors, and with no body weight loss or other signs of toxicity in mice. BETd-260 (5 mg/kg, i.v.) degrades the BRD2, BRD3, and BRD4 proteins for more than 24 h, with robust cleavage of PARP and caspase-3, and strong down-regulation of c-Myc protein in RS4;11 xenograft mice model.
Price1080$
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