PROTAC PARP1 degrader-4

Name: PROTAC PARP1 degrader-4
Brand: TargetMol
SKU: T204787
Rating: 4.5 (1 reviews)

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Catalog No. T204787

PROTAC PARP1 degrader-4 (Compound 180055) is a selective PARP1 PROTAC degrader, demonstrating DC50 values of 180 nM and 240 nM in T47D and MDA-MB-231 cell lines, respectively. It facilitates the ubiquitination and degradation of PARP1 and inhibits its enzymatic activity without causing significant DNA trapping effects. Additionally, PROTAC PARP1 degrader-4 can inhibit tumors with BRCA gene mutations while having minimal impact on the growth of normal cells.

PROTAC PARP1 degrader-4

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Catalog No. T204787

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Product Introduction

Bioactivity

Description	PROTAC PARP1 degrader-4 (Compound 180055) is a selective PARP1 PROTAC degrader, demonstrating DC50 values of 180 nM and 240 nM in T47D and MDA-MB-231 cell lines, respectively. It facilitates the ubiquitination and degradation of PARP1 and inhibits its enzymatic activity without causing significant DNA trapping effects. Additionally, PROTAC PARP1 degrader-4 can inhibit tumors with BRCA gene mutations while having minimal impact on the growth of normal cells.
In vitro	PROTAC PARP1 degrader-4 (1-10 μM, 24-48 h) shields T47D and MOLT4 cells from cell death induced by genotoxic stress [1]. Additionally, PROTAC PARP1 degrader-4 (10 μM, 3-6 days) induces cytotoxic effects in BRCA1-mutated MOLT4 cells [1].
In vivo	PROTAC PARP1 degrader-4 (40 mg/kg, intraperitoneal injection, 16 days) exhibits antitumor activity against MOLT4 xenograft mice with BRCA1 mutations [1].

Chemical Properties

Molecular Weight	920.145
Formula	C₅₁H₆₂FN₇O₆S

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice./Shipping at ambient temperature.

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

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