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BETd-260

Catalog No. T14550Cas No. 2093388-62-4
Alias ZBC 260

BETd-260, a PROTAC linked by a Cereblon ligand and a BET ligand, has an inhibitory effect on BRD4 protein in leukemic cell lines.

BETd-260

BETd-260

Purity: 96.76%
Catalog No. T14550Alias ZBC 260Cas No. 2093388-62-4
BETd-260, a PROTAC linked by a Cereblon ligand and a BET ligand, has an inhibitory effect on BRD4 protein in leukemic cell lines.
Pack SizePriceAvailabilityQuantity
1 mg$132In Stock
5 mg$328In Stock
10 mg$496In Stock
25 mg$786In Stock
50 mgInquiryIn Stock
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Purity:96.76%
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Product Introduction

Bioactivity
Description
BETd-260, a PROTAC linked by a Cereblon ligand and a BET ligand, has an inhibitory effect on BRD4 protein in leukemic cell lines.
Targets&IC50
BRD2:30-100 pM, BRD3:30-100 pM, BRD:0.0022 μM, BRD4:<30 pM
In vitro
betd - 260 (ZBC260; Compound 23) induced the degradation of BRD2, BRD3 and BRD4 proteins. BETd-260 acted on RS4; The ic50 measured for 11 leukemic cells was 51 pM. The ic50 of BETd-260 in MOLM-13 cells was 2.2 nM. BETd-260 at 3-10 nM could induce RS4; 11 and MOLM-13 cell apoptosis. Moreover, BETd-260 inhibited the transcription and translation of anti-apoptotic genes Mcl-1, Bcl-2, c-Myc and XIAP and increased the transcription and translation of pro-apoptotic gene Bad in HCC cells[1].
In vivo
BETd-260, administered intravenously at a dosage of 5 mg/kg, effectively degrades the proteins BRD2, BRD3, and BRD4, maintaining this activity for over 24 hours. This process is accompanied by significant PARP and caspase-3 cleavage, along with a marked reduction in c-Myc protein levels in the RS4;11 xenograft mouse model[1]. When administered bi-weekly, three times a week for three weeks, BETd-260 induces rapid tumor regression, achieving a peak regression greater than 90% in RS4;11 xenograft tumor-bearing mice. Notably, this treatment regimen does not lead to weight loss or other toxicity symptoms in the mice.
AliasZBC 260
Chemical Properties
Molecular Weight798.89
FormulaC43H46N10O6
Cas No.2093388-62-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 22.5 mg/mL (28.2 mM), Sonication is recommended.
H2O: 0.1 mg/mL, insoluble
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.2517 mL6.2587 mL12.5174 mL62.5868 mL
5 mM0.2503 mL1.2517 mL2.5035 mL12.5174 mL
10 mM0.1252 mL0.6259 mL1.2517 mL6.2587 mL
20 mM0.0626 mL0.3129 mL0.6259 mL3.1293 mL

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