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ZXH-4-130 TFA

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Catalog No. T77920Cas No. 2711006-67-4

ZXH-4-130 TFA is a hetero-PROTAC (CRBN-VHL compound) that efficaciously and selectively mediates the degradation of CRBN, achieving approximately 80% degradation at a concentration of 10 nM in MM1.S cells [1].

ZXH-4-130 TFA

ZXH-4-130 TFA

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Catalog No. T77920Cas No. 2711006-67-4
ZXH-4-130 TFA is a hetero-PROTAC (CRBN-VHL compound) that efficaciously and selectively mediates the degradation of CRBN, achieving approximately 80% degradation at a concentration of 10 nM in MM1.S cells [1].
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Product Introduction

Bioactivity
Description
ZXH-4-130 TFA is a hetero-PROTAC (CRBN-VHL compound) that efficaciously and selectively mediates the degradation of CRBN, achieving approximately 80% degradation at a concentration of 10 nM in MM1.S cells [1].
In vitro
ZXH-4-130 TFA at a concentration of 100 nM and pre-treatment for 2 hours significantly inhibited the cytotoxic effects of pomalidomide (1 μM) when cells were subsequently treated for 96 hours, displaying a statistically significant protective effect [1]. Additionally, a pre-treatment with ZXH-4-130 TFA at 50 nM was able to rescue the degradation of GSPT1 in MM1.S cells induced by CC-885 [1]. Furthermore, ZXH-4-130 TFA (100 nM; pre-treated for 2 hours, followed by treatment with THAL-SNS-032 for 6 hours) nearly completely induced the degradation of CRBN, whereas THAL-SNS-032 only partially inhibited CDK9 activity [1].
Chemical Properties
Molecular Weight985.08
FormulaC48H59F3N6O11S
Cas No.2711006-67-4
SmilesC(C(O)=O)(F)(F)F.O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2OCCCCCCCCCCC(N[C@H](C(=O)N4[C@H](C(NCC5=CC=C(C=C5)C=6SC=NC6C)=O)C[C@@H](O)C4)C(C)(C)C)=O
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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