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KT-333 ammonium

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Catalog No. T86788Cas No. 2839758-34-6

KT-333 ammonium (Compound A) acts as a molecular glue that targets and promotes the degradation of the STAT3 protein through the ubiquitin-proteasome system. This compound achieves selective degradation by binding simultaneously to the STAT3 protein and the E3 ubiquitin ligase von Hippel-Lindau protein (VHL). It exhibits strong selectivity and efficacy in degrading STAT3, possessing notable antitumor properties. KT-333 ammonium is particularly useful for research on hematologic malignancies, including large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) [1].

KT-333 ammonium
Other Forms of KT-333 ammonium:

KT-333 ammonium

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Catalog No. T86788Cas No. 2839758-34-6
KT-333 ammonium (Compound A) acts as a molecular glue that targets and promotes the degradation of the STAT3 protein through the ubiquitin-proteasome system. This compound achieves selective degradation by binding simultaneously to the STAT3 protein and the E3 ubiquitin ligase von Hippel-Lindau protein (VHL). It exhibits strong selectivity and efficacy in degrading STAT3, possessing notable antitumor properties. KT-333 ammonium is particularly useful for research on hematologic malignancies, including large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) [1].
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Product Introduction

Bioactivity
Description
KT-333 ammonium (Compound A) acts as a molecular glue that targets and promotes the degradation of the STAT3 protein through the ubiquitin-proteasome system. This compound achieves selective degradation by binding simultaneously to the STAT3 protein and the E3 ubiquitin ligase von Hippel-Lindau protein (VHL). It exhibits strong selectivity and efficacy in degrading STAT3, possessing notable antitumor properties. KT-333 ammonium is particularly useful for research on hematologic malignancies, including large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) [1].
In vitro
KT-333 ammonium, at a concentration of (11.8±2.3 nM over 48 hours), causes irreversible growth inhibition and induces the activity of caspase 3/7, a marker of apoptosis, in the SU-DHL-1 cell line following STAT3 degradation [1]. Additionally, KT-333 ammonium demonstrates STAT3 protein degradation with GI50 values ranging from 8.1 to 57.4 nM across various ALCL cell lines in cell phenotype analysis [1].
In vivo
KT-333 ammonium exhibited dose-dependent antitumor activity when administered intravenously at doses of 5, 10, 15, and 45 mg/kg once weekly for two weeks. Mice receiving 5 mg/kg showed 79.9% tumor growth inhibition (TGI), while doses of 10, 15, or 45 mg/kg led to complete tumor regression, sustained until the study's conclusion [1]. Similarly, doses of 10, 20, and 30 mg/kg resulted in dose-dependent antitumor effects, with mice given 10 mg/kg achieving 83.8% TGI, and those receiving 20 or 30 mg/kg experiencing complete tumor regression, also persisting through to the end of the study [1].
Chemical Properties
Molecular Weight1274.81
FormulaC60H77ClN11O14PS
Cas No.2839758-34-6
SmilesClC(C(CCCC(N[C@@H](C(C)(C)C)C(N1[C@@H](C[C@H](C1)O)C(N[C@H](C2=CC=C(C3=C(N=CS3)C)C=C2)C)=O)=O)=O)=CC=C4)=C4OC[C@H](CCC(N)=O)NC([C@H]5N6[C@](CCN(C[C@@H](C6=O)NC(C7=CC8=CC(C(P(O)([O-])=O)=O)=CC=C8N7)=O)C(C)=O)([H])CC5)=O.[NH4+]
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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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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