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SIAIS100 TFA

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Catalog No. T77969

SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with a DC50 of 2.7 nM, used in chronic myeloid leukemia (CML) research [1].

SIAIS100 TFA

SIAIS100 TFA

Copy Product Info
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Catalog No. T77969
SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with a DC50 of 2.7 nM, used in chronic myeloid leukemia (CML) research [1].
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with a DC50 of 2.7 nM, used in chronic myeloid leukemia (CML) research [1].
In vitro
SIAIS100 exhibits antiproliferative activity against K562 cells with an IC50 value of 12 nM [1]. It induces degradation of BCR-ABL by 81.78% and 91.20% at concentrations of 5 nM and 100 nM, respectively [1]. SIAIS100 (100 nM; 8 h) significantly decreases BCR-ABL in K562 cells [1]. SIAIS100 (100 nM; 6 h) causes persistent and robust degradation of BCR-ABL, maintaining a durable cellular response post drug removal [1]. Additionally, SIAIS100 (1-1000 nM) significantly reduces mutant G250E/T315I in a dose-dependent manner and inhibits BCR-ABL signaling in 32D cells, as assessed by p-BCR-ABL levels [1].
Chemical Properties
Molecular Weight1004.46
FormulaC46H51ClF5N9O7S
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:
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2 Enter the in vivo formulation:
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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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